81377-02-8
Chemical Structure
Seglitide
Synonym(s): MK-678; L-363586
- CAS No.: 81377-02-8
- Formula:C44H56N8O7
- Molecular Weight:808.96
IUPAC Name: (3S,6S,9S,12R,15S,18S)-12-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-3-benzyl-15-(4-hydroxybenzyl)-6-isopropyl-1,18-dimethyl-1,4,7,10,13,16-hexaazacyclooctadecane-2,5,8,11,14,17-hexaone
InChIKey: NPJIOCBFOAHEDO-AVWFULIKSA-N
SMILES: O=C([C@@H](NC([C@@H](N(C([C@@H](NC([C@@H](NC([C@@H](NC1=O)CCCCN)=O)C(C)C)=O)CC2=CC=CC=C2)=O)C)C)=O)CC3=CC=C(C=C3)O)N[C@@H]1CC4=CNC5=CC=CC=C45
Biological Activity: Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus[1][2][3][4].
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Seglitide | 99.30% | Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus. | ||||||||||||||||||||
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- [1]. Dimech J, et al. Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria. Br J Pharmacol. 1993;109(4):898-899. [Content Brief]
- [2]. Hartmann J, et al. Blood pressure reduction in hypertensive-diabetic rats by the somatostatin analog MK-678. Life Sci. 1989;45(3):267-274. [Content Brief]
- [3]. Bhattarai JP, et al. Somatostatin inhibition of gonadotropin-releasing hormone neurons in female and male mice. Endocrinology. 2010 Jul;151(7):3258-66. [Content Brief]
- [4]. McKeen ES, et al. Mediation by SRIF1 receptors of the contractile action of somatostatin in rat isolated distal colon; studies using some novel SRIF analogues. Br J Pharmacol. 1994;113(2):628-634. [Content Brief]
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