GRGDSPC, a 7-amino acid peptide, is a thiolated cell adhesion peptide[1].
体外研究 (In Vitro)
GRGDSPC is conjugated to acrylated dextran via thiol-acrylate reaction to regulate the interactions of human mesenchymal stem cells (hMSCs) with the photocrosslinkable hydrogels. To determine the conjugation kinetics and efficiency of GRGDSPC peptide to DEX-MAES16, various GRGDSPC concentrations (i.e., 5, 10 and 20 mg/1 g DEX-MAES16) are conjugated to the acrylated Dextran (DEX) macromer over time (0.25, 0.5, 1 and 3h) in PBS at pH 7.8 and the free thiol groups of unreacted peptides are quantified using Ellman’s assay. In addition, the reaction kinetics of the thiol-peptide to acrylated (DEX-MAES16) and methacrylated (DEX-HEMA16) macromers are compared. As early as 15 min conjugation, with 5, 10 and 20 mg of GRGDSPC peptide/1 g modified DEX, the peptide conjugation efficiencies with DEX-MAES are 105.40, 94.10 and 87.45%, respectively, while for the reaction with the DEX-HEMA they are 0.73, 15.78 and 18.42%, respectively. After 1h, the GRGDSPC conjugation with DEX-MAES is completed with the peptide concentration of 10 mg, but only 35.66% of the thiol groups of the peptide react with DEX-HEMA. The reaction kinetics are also monitored at 3 h of conjugation, and all of the 20 mg GRGDSPC peptide reacts with acrylated DEX compared to only 32.53% for the methacrylated DEX at this time point[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
690.73
Formula
C25H42N10O11S
CAS 号
91575-26-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Nguyen MK, et al. Photocrosslinkable, biodegradable hydrogels with controlled cell adhesivity for prolonged siRNAdelivery to hMSCs to enhance their osteogenic differentiation. J Mater Chem B. 2017 Jan 21;5(3):485-495.
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
IC50 Target
Ki: 20-30 nM (kappa3 opioid receptor)[1]
体外研究 (In Vitro)
Endomorphin 2 is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 1 (EM-2). The two Endomorphins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ1 and μ2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
571.67
Formula
C32H37N5O5
CAS 号
141801-26-5
Sequence
Tyr-Pro-Phe-Phe-NH2
Sequence Shortening
YPFF-NH2
中文名称
内吗啡肽 2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.
Kinase Assay [1]
125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2 nM) is performed in potassium phosphate buffer (50 mM, pH 7.4; 0.5 mL) with MgCl2 (5 mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06 mg protein/mL for MOR-1/CHO cells. Specific binding is determined in the presence and absence of either 1 μM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25°C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethylenimine and washed twice with ice cold Tris buffer using a Brandel cell harvester. The filters are then counted on a Packard Cobra gamma counter. The other opioid receptor binding assays are performed[1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Mice[1] Groups of mice are treated i.c.v. with Endomorphin 1 (12 μg) or Endomorphin 2 (3 μg) 15 min before a 0.5-cc charcoal meal (2.5% gum tragacanth,10% activated charcoal in water). The mice are killed 30 min later and the distance the charcoal traveled is measured.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.
[1]. Kim JW, et al. Triterpenoid Saponins Isolated from Platycodon grandiflorum Inhibit Hepatitis C Virus Replication. Evid Based Complement Alternat Med. 2013;2013:560417.
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects[1][2][3][4][5][6].
IC50 Target
IC50: 20 nM (Complement C5a receptor)[4] MrgX2[1]
体外研究 (In Vitro)
PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively[1]. PMX-53 (10 nM) inhibits C5a-induced Ca2+ mobilization in HMC-1 cells, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34+ cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg abolishes the ability of PMX-53 to inhibit C5a-induced Ca2+ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
PMX-53 (0.3-3 mg/kg; subcutaneous injection; once; male Wistar rats) treatment inhibits the hypernociception induced by zymosan-activated serum and C5a but not by the direct-acting hypernociceptive mediators, prostaglandin E2 and dopamine[2]. Local pretreatment of rats with PMX-53 (60-180 μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception[2]. Pharmacokinetic analyses have shown that PMX-53 (3D53) appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 µM beingreached within 20 min The plasma elimination half-life wasapproximately 70 min in this case[3]. The non-acetylated version of PMX-53 (3D53) binds to isolated mouse neutrophils with a Kd value of 30 nM (mouse C5a binds with a Kd value of 0.3 nM) and inhibits mouse C5a-induced chemotaxis with an IC50 value of 0.5 nM[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Adult male Wistar rats (weighing 180-200 g) injected with zymosan[2]
Dosage:
0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration:
Subcutaneous injection; once
Result:
Inhibited the hypernociception induced by zymosan-activated serum and C5a.
分子量
896.09
Formula
C47H65N11O7
CAS 号
219639-75-5
Sequence Shortening
F-{Orn}-P-{d-Cha}-WR (Lactam bridge: Orn2- Arg6)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Protect from light, stored under nitrogen
Powder
-80deg;C
2 years
-20deg;C
1 year
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;
DMSO : 125 mg/mL (139.49 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.1160 mL
5.5798 mL
11.1596 mL
5 mM
0.2232 mL
1.1160 mL
2.2319 mL
10 mM
0.1116 mL
0.5580 mL
1.1160 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13.
[2]. Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53.
[3]. Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73.
[4]. Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74.
[5]. Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25(7):2447-55.
[6]. Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74(13):3454-65.
[1]. Li W, et al. Platycoside N: a new oleanane-type triterpenoid saponin from the roots of Platycodon grandiflorum. Molecules. 2010 Nov 30;15(12):8702-8.
5-PAHSA-d9 is the deuterium labeled 5-PAHSA. 5-PAHSA is a kind of anti-inflammatory and antidiabetic lipokines that connect glucose and lipid metabolism[1].
分子量
547.94
Formula
C34H57D9O4
CAS 号
1809226-17-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Veronika Paluchova, et al. Lipokine 5-PAHSA Is Regulated by Adipose Triglyceride Lipase and Primes Adipocytes for De Novo Lipogenesis in Mice. Diabetes. 2020 Mar;69(3):300-312.
[1]. Kim YS, et al. Isolation of a new saponin and cytotoxic effect of saponins from the root of Platycodon grandiflorum on human tumor cell lines. Planta Med. 2005 Jun;71(6):566-8.
D149 Dye is an indoline-based dye, which is a high-extinction-coefficient metal-free organic sensitizer.
体外研究 (In Vitro)
D149 is a metal-free organic dye, which is promising all-organic alternatives. D149 displays power conversion efficiency of up to 9%. Furthermore, D149 has a peak extinction co-efficient of 68700 M-1 cm-1 at 540 nm, significantly higher than 13900 M-1cm-1 at 535 nm for N719[1]. D149, a metal-free indoline dye, is one of the most promising sensitizers for dye-sensitized solar cells (DSSCs) and has shown very high solar energy conversion efficiencies of 9%. D149 shows a large number of unresolved aromatic and olefinic signals between 7 and 7.5 ppm[2]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
741.94
Formula
C42H35N3O4S3
CAS 号
786643-20-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lin J, et al. 3D hierarchical rutile TiO2 and metal-free organic sensitizer producing dye-sensitized solar cells 8.6% conversion efficiency. Sci Rep. 2014 Aug 29;4:5769.
[2]. El-Zohry A, et al. Isomerization and Aggregation of the Solar Cell Dye D149. J Phys Chem C Nanomater Interfaces. 2012 Dec 20;116(50):26144-26153.
Cell Assay [1]
The porous TiO2 films are immersed in a 0.5 mM D149 (1-material) dye solution in a 1:1 (v/v) mixture of acetonitrile (HPLC) and tert-butanol (LR) overnight once their temperature decreased to approximately 110°C. The samples are then taken out of the dye bath, washed with acetonitrile, and dried. The working electrode and Pt counter electrode [produced using a pre-drilled piece of 2.3 mm FTO glass, coated with one drop of 10 mM platinic acid solution [H2PtCl6] and heated to 400°C for 20 min] are assembled into a sandwich type cell and sealed with a spacer of 25 μm Surlyn. An I-1/I3-1 organic solvent based electrolyte solution [50 mM iodine, 0.6 M 1,2-dimethyl-3-propylimidazelium iodide, 0.1 M lithium iodide in methoxypropionitrile] is introduced via vacuum back-filling. The hole is sealed with a piece of aluminium foil-backed Surlyn[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Lin J, et al. 3D hierarchical rutile TiO2 and metal-free organic sensitizer producing dye-sensitized solar cells 8.6% conversion efficiency. Sci Rep. 2014 Aug 29;4:5769.
[2]. El-Zohry A, et al. Isomerization and Aggregation of the Solar Cell Dye D149. J Phys Chem C Nanomater Interfaces. 2012 Dec 20;116(50):26144-26153.
