[Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
IC50 Target
δ and ζ opioid receptor[1]
体外研究 (In Vitro)
[Met5]-Enkephalin at 0.1 nM, 10 nM, and 1 μM significantly reduces the total number of glial cells in culture[1]. [Met5]-Enkephalin, amide acts via δ-opioid receptor to inhibit pelvic nerve-evoked contractions of cat distal colon. [Met5]-enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC50 value of 2.2 nM. [Met5]enkephalin at a concentration (3 nM) which produces a large inhibition of neurogenic contractions, has no effect on contractions to exogenous acetylcholine[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
686.70
Formula
C29H37F3N6O8S
Sequence
Tyr-Gly-Gly-Phe-Met-NH2
Sequence Shortening
YGGFM-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Stiene-Martin A, et al. Glial growth is regulated by agonists selective for multiple opioid receptor types in vitro. J Neurosci Res. 1991 Aug;29(4):538-48.
[2]. Kennedy C, et al. [Met5]enkephalin acts via delta-opioid receptors to inhibit pelvic nerve-evoked contractions of cat distal colon. Br J Pharmacol. 1987 Oct;92(2):291-8.
GLP-1(7-36), amide TFA is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells[1].
体外研究 (In Vitro)
Cells treated with phorbol 12-myristate 13-acetate for 2 h has significantly higher active GLP-1(7-36) Acetate (Human GLP-1-(7-36)-amide Acetate) concentrations in the media than those in the control. The glucose treatment also increases active GLP-1 secretion from cells in dose-dependent manner. Palmitic, oleic, linoleic or linolenic acid dose-dependently stimulated active GLP-1 secretion from cells. Active GLP-1 secretion is significantly greater with unsaturated fatty acids such as oleic, linoleic and linolenic acids than with palmitic acid. The treatment of NCI-H716 cells with CPE dose-dependently increases active GLP-1 concentrations in the media. A 37% increase is observed in active GLP-1 secretion from these cells at a concentration of 0.1 % CPE[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Gastric administration of glucose increases active GLP-1(7-36) amide levels in the portal blood after 10 min, followed by a marked decrease at 30 min. The gastric administration of TO also increases active GLP-1 levels after 10 min, and followed by a decrease to basal levels at 60 min. Individually, glucose and TO increase the secretion of GLP-1 in a dose-dependent manner. Furthermore, the co-administration of glucose and TO additively increase peak GLP-1 levels. CPE-administered mice have higher active GLP-1 levels in the portal blood at 10 and 30 min than those in the control mice. When glucose is administered with CPE, active GLP-1 and insulin levels in the portal blood are slightly higher in CPE-administered mice than in the control mice. High-fat diet-fed C57BL/6J mice develop hyperglycaemia and impair glucose tolerance[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
3411.65
Formula
C151H227F3N40O47
Sequence Shortening
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRNH2
运输条件
Room temperature in continental US; may vary elsewhere.
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]. Fujii Y et al. Ingestion of coffee polyphenols increases postprandial release of the active glucagon-like peptide-1(GLP-1(7-36)) amide in C57BL/6J mice. J Nutr Sci. 2015 Mar 3;4:e9.
GRF (1-29) amide (rat) is a synthetic peptide which can stimulate the growth hormone (GH) secretion.
体内研究 (In Vivo)
Time course studies of GRF (1-29) amide (rat) disappearance show apparent half-lives of 18±4 min and 13±3 min in serum and liver homogenate, respectively. This is accompanied by the appearance of degradation products that are all less hydrophobic than the native peptide. In the serum, two major metabolites are detected and isolated by preparative HPLC[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Boulanger L, et al. Catabolism of rat growth hormone-releasing factor(1-29) amide in rat serum and liver. Peptides. 1992 Jul-Aug;13(4):681-9.
Cell Assay [1]
To isolate GRF metabolites in the liver, rGRF(1-29)NH2 (10 mg) is first preincubated in 232 mL of Krebs’ buffer (5 min, 37°C) to help GRF solubilization and then incubated with a liver homogenate in a shaking bath at 37°C. The homogenate is prepared as in the degradation assays with 580 mg of liver (10 mg/mL). The reaction is stopped after 30 min by adding 174 mL of cold 50 mM phosphate solution (pH 0.8) and centrifugation (48,000×g, 20 min, 4°C). The supernatant is filtered twice and its pH is adjusted (3.0) with 6 N NaOH before chromatography. The GRF metabolites and residual rGRF(1-29)NH2 are isolated[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Boulanger L, et al. Catabolism of rat growth hormone-releasing factor(1-29) amide in rat serum and liver. Peptides. 1992 Jul-Aug;13(4):681-9.
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42)[1]. GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
[1]. L S Hansen, et al. N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor. Br J Pharmacol. 2016 Mar;173(5):826-38.
![[Met5]-Enkephalin, amide TFAamp;;(Synonyms: 5-Methionine-enkephalin amide TFA)](http://file.medchemexpress.cn/product_pic/hy-p1467a.gif "[Met5]-Enkephalin, amide TFA Chemical Structure")
