2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. Seglitide

Seglitide  (Synonyms: MK-678; L-363586)

製品番号: HY-106103 純度: 99.30%
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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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Seglitide

Seglitide 構造式

CAS 番号 : 81377-02-8

容量 価格（税別） 在庫状況 数量
1 mg $110 在庫あり
5 mg $270 在庫あり
10 mg $420 在庫あり
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製品説明

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].

IC50 & Target[1]

SSTR2

 

体内実験

Seglitide (50-1000 µg/rat/day; p.o.; daily; up to 49 days) produces a reversible, sustained 11-21% reduction in systolic blood pressure in Streptozotocin (HY-13753)-induced hypertensive diabetic male Sprague-Dawley rats, with no effect on relevant hormones, renin-angiotensin system components, blood glucose, or growth rate[2].
Seglitide (50-100 µg/rat/day; p.o.; daily; 49 days) produces only a transient 11% reduction in systolic blood pressure in male spontaneously hypertensive rats, with no sustained hypotensive effect, and no impact on relevant hormones, renin-angiotensin system components, blood glucose, or growth rate[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, streptozotocin-induced diabetic hypertension)[2]
Dosage: 50 µg/rat/day (days 1-20); 100 µg/rat/day (days 21-49); 1000 µg/rat/day; 100 µg (acute parenteral)
Administration: p.o. (via drinking water, days 1-20); p.o. (via drinking water, days 21-49); p.o. (unspecified duration); parenteral (single acute dose)
Result: Reduced systolic blood pressure of diabetic rats by 14% after 17 days of 50 µg/rat/day treatment (P=0.05).
Maintained systolic blood pressure significantly reduced by 11-21% relative to untreated diabetic rats over days 24-49 with 100 µg/rat/day dose, matching normotensive control levels (98-118 mmHg; repeated measures ANOVA, P<0.003 vs. untreated diabetic rats, P=0.687 vs. normal rats).
Reversed hypotensive effect 5 days after drug withdrawal, with only a 6% reduction in blood pressure (nsd).
Showed no significant effect on plasma renin activity, angiotensin converting enzyme activity, or aldosterone levels in diabetic rats.
Did not alter circulating insulin or glucagon levels in diabetic rats with 1000 µg/rat/day oral dose, but reduced circulating insulin levels by 44% with acute parenteral 100 µg dose (P<0.05).
Had no significant effect on blood glucose levels or growth rate of diabetic rats over 49 days of treatment.
Animal Model: Spontaneously hypertensive (SH) (male)[2]
Dosage: 50 µg/rat/day (days 1-40); 100 µg/rat/day (days 41-49)
Administration: p.o. (via drinking water, days 1-40); p.o. (via drinking water, days 41-49)
Result: Reduced systolic blood pressure of SH rats by 11% at the 10-day time point (P<0.02), with no significant blood pressure reduction observed in subsequent measurements even after dose escalation to 100 µg/rat/day.
Showed no significant effect on plasma renin activity, angiotensin converting enzyme activity, or aldosterone levels in SH rats.
Did not alter blood glucose levels or growth rate of SH rats over 49 days of treatment.
分子量

808.96

分子式

C44H56N8O7
CAS 番号
Appearance

Solid

Color

White to off-white

Sequence

Cyclo({Ala(Me)}-Tyr-{d-Trp}-Lys-Val-Phe)
Sequence Shortening

Cyclo({Ala(Me)}-Y-{d-Trp}-KVF)
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Sealed storage, away from moisture
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
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参考文献
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Keywords:

Seglitide81377-02-8MK-678 L-363586MK678MK 678L363586L 363586L-363586Somatostatin ReceptorSSTRsSSTRspontaneously hypertensive ratsguinea-pig isolated right atriasomatostatin receptor subtype 2GnRH neuronscarbacholN6-cyclohexyladenosinestreptozotocin-diabetic ratsfemale micemale micerat isolated distal colonInhibitorinhibitorinhibit

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Seglitide
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HY-106103
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