L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic[1][2].
IC50 Target
TRPV1
0.1 mu;M (IC50)
分子量
1128.21
Formula
C48H72F3N21O8
Sequence Shortening
RRRRWW-NH2
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]. Planells-Cases R, et, al. Arginine-rich peptides are blockers of VR-1 channels with analgesic activity. FEBS Lett. 2000 Sep 15; 481(2): 131-6.
[2]. Himmel HM, et, al. The arginine-rich hexapeptide R4W2 is a stereoselective antagonist at the vanilloid receptor 1: a Ca2+ imaging study in adult rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 2002 Jun; 301(3): 981-6.
L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic[1][2].
IC50 Target
TRPV1
0.1 mu;M (IC50)
分子量
1014.19
Formula
H2NW2
CAS 号
206350-79-0
Sequence Shortening
RRRRWW-NH2
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]. Planells-Cases R, et, al. Arginine-rich peptides are blockers of VR-1 channels with analgesic activity. FEBS Lett. 2000 Sep 15; 481(2): 131-6.
[2]. Himmel HM, et, al. The arginine-rich hexapeptide R4W2 is a stereoselective antagonist at the vanilloid receptor 1: a Ca2+ imaging study in adult rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 2002 Jun; 301(3): 981-6.
Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research[1].
体外研究 (In Vitro)
Atosiban inhibits the oxytocin-mediated release of IP3 from the myometrial cell membrane. There is reduced release of intracellular, stored calcium from the sacroplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
The posterior pituitary hormones, oxytocin and arginine vasopressin, differ in structure by only two amino acids, and Atosiban influences physiological effects of arginine vasopressin on the feto-maternal cardiovascular and renal systems. In late-gestation sheep, the administration of Atosiban for 1 hour fails to induce fetomaternal cardiovascular changes[1]. Atosiban blocks the activation of oxytocin-receptor-expressing neurons in the parabrachial nucleus of mice[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
1054.24
Formula
C45H71N11O14S2
CAS 号
914453-95-5
中文名称
醋酸阿托西班
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 : 100 mg/mL (94.86 mM; Need ultrasonic)
H2O : 50 mg/mL (47.43 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.9486 mL
4.7428 mL
9.4855 mL
5 mM
0.1897 mL
0.9486 mL
1.8971 mL
10 mM
0.0949 mL
0.4743 mL
0.9486 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]. Sanu O, et al. Critical appraisal and clinical utility of atosiban in the management of preterm labor. Ther Clin Risk Manag. 2010 Apr 26;6:191-9.
[2]. Philip J Ryan, et al. Oxytocin-receptor-expressing Neurons in the Parabrachial Nucleus Regulate Fluid Intake. Nat Neurosci. 2017 Dec;20(12):1722-1733.