SSTR5 antagonist 1|cas:1628741-91-2|西域试剂

SSTR5 antagonist 1,99.84%

产品编号：Bellancom-102037| CAS NO：1628741-91-2| 分子式：C₂₈H₃₄FN₃O₅| 分子量：511.59

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货号	价格	库存与货期
Bellancom-102037	￥3500.00	杭州北京（现货）
Bellancom-102037	￥5500.00	杭州北京（现货）
Bellancom-102037	￥9900.00	杭州北京（现货）
Bellancom-102037	￥16500.00	杭州北京（现货）
Bellancom-102037	￥22500.00	杭州北京（现货）

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SSTR5 antagonist 1

产品介绍

SSTR5 antagonist 1 (compound 25a) 是一种选择性，口服有效的生长抑素受体亚型 5 (SSTR5) 拮抗剂，对 hSSTR5 和 mSSTR5 的 IC₅₀ 分别为 9.6 和 57 nM。

生物活性

SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC₅₀s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.

体外研究

SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%.
SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%.
SSTR5 antagonist 1 (1 μM; 15 min and 30 min) exhibits good metabolic stability toward both human and mouse microsomes with in vitro CLint value of <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

SSTR5 antagonist 1 (compound 25a) (1 mg/kg; p.o.; single dose) is orally available with acceptable plasma exposure in mice in pharmacokinetic screening and exhibits excellent solubility (260 μg/mL, pH=6.8).
SSTR5 antagonist 1 (100 mg/kg; p.o.; single dose; measured at 0-120 min) augments insulin secretion in a glucose-dependent manner and lowers blood glucose concentration in high-fat diet fed C57BL/6J mice.
SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; p.o.; single dose) shows dose-dependent effect on glucose excursion measured during the oral glucose tolerance test in HFD fed C57BL/6J mice.
Pharmacokinetic profiles in male ICR mouse (8-week-old)

Route	Dose (mg/kg)	CL_total (mL/h/kg)	V_ss (mL/kg)	MRT (h)
iv	0.1	1761	3052	1.7	/
Route	Dose (mg/kg)	C_max (ng/mL)	T_{max (h)}	AUC_{0-8 h (ng·h/mL)}	F (%)
po	1	74.8	2.0	332	58

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	High-fat diet fed C57BL/6J mice
Dosage:	100 mg/kg
Administration:	Oral gavage; single dose; monitored over 2 h
Result:	Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide (HY-15206) and comparable to that of 30 mg/kg Alogliptin (HY-A0023A). Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.

体内研究

Route	Dose (mg/kg)	CL_total (mL/h/kg)	V_ss (mL/kg)	MRT (h)
iv	0.1	1761	3052	1.7	/
Route	Dose (mg/kg)	C_max (ng/mL)	T_{max (h)}	AUC_{0-8 h (ng·h/mL)}	F (%)
po	1	74.8	2.0	332	58

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	High-fat diet fed C57BL/6J mice
Dosage:	100 mg/kg
Administration:	Oral gavage; single dose; monitored over 2 h
Result:	Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide (HY-15206) and comparable to that of 30 mg/kg Alogliptin (HY-A0023A). Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 90 mg/mL (175.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9547 mL	9.7735 mL	19.5469 mL
5 mM	0.3909 mL	1.9547 mL	3.9094 mL
10 mM	0.1955 mL	0.9773 mL	1.9547 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。-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：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。