Cofrogliptin HSK7653|cas:1844874-26-5|西域试剂

Cofrogliptin HSK7653,99.07%

产品编号：Bellancom-147257| CAS NO：1844874-26-5| 分子式：C₁₈H₁₉F₅N₄O₃S| 分子量：466.43

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-147257		￥4800.00	杭州北京（现货）
Bellancom-147257		￥8000.00	杭州北京（现货）

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Cofrogliptin HSK7653

产品介绍

Cofrogliptin (HSK7653) (compound 2)，一种四氢吡喃衍生物，是一种有效的口服 DPP-4 抑制剂，具有长效降糖作用。Cofrogliptin (compound 2) 在2型糖尿病 (T2DM) 应用中具有很大的潜力。

生物活性

Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .

体外研究

Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC₅₀ value of 4.18 nM.

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

体内研究

Cofrogliptin (HSK7653) (compound 2) (IV: 0.5 mg/kg; PO: 2 mg/kg) exhibits extremely long half-lives and low rate of reduction of drug concentration after orally administration.
Cofrogliptin (compound 2) (Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg) increases of half-lives, has high oral exposure, low i.v. clearance and hepatic microsomal clearance after intravenous dosing.
Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) exhibits longe inhibition time of DPP-4 and decreases HbA1c level at the doses of 3 and 10 mg/kg in ob/ob mice. Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) also has a great potential of biweekly regimen for T2DM as indicated in rhesus monkeys.

Pharmacokinetic Parameters in ICR mice

	IV(dose: 0.5 mg/kg)			PO(dose: 2 mg/kg)
	CI(mL/min/kg)	V_dss(L/kg)	t_1/2(h)	C_max(ng/mL)	t_1/2(h)	AUC_0-t(ng•h/mL)	F%
Omarigliptin	7.39±2.1	1.65±0.27	3.05±0.6	798±122	4.65±1.4	4095±552	95.0±29
Cofrogliptin (compound 2)	2.57±0.09	3.30±0.33	25.6±9.6	352±20	29.9±3.2	7898±873	62.2±6.9

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

Animal Model:	ob/ob mice
Dosage:	3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:	Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg
Result:	Exhibited strong inhibition capability of plasma DPP-4 in a dose dependent manner.

Animal Model:	rhesus monkeys
Dosage:	10 mg/kg
Administration:	Single, orally, 10 mg/kg
Result:	Possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days. Remained the plasma DPP-4 inhibition rates of 76.16% and 43.41%, respectively at the end of second week and third week after administration.

体内研究

	IV(dose: 0.5 mg/kg)			PO(dose: 2 mg/kg)
	CI(mL/min/kg)	V_dss(L/kg)	t_1/2(h)	C_max(ng/mL)	t_1/2(h)	AUC_0-t(ng•h/mL)	F%
Omarigliptin	7.39±2.1	1.65±0.27	3.05±0.6	798±122	4.65±1.4	4095±552	95.0±29
Cofrogliptin (compound 2)	2.57±0.09	3.30±0.33	25.6±9.6	352±20	29.9±3.2	7898±873	62.2±6.9

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

Animal Model:	ob/ob mice
Dosage:	3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:	Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg
Result:	Exhibited strong inhibition capability of plasma DPP-4 in a dose dependent manner.

Animal Model:	rhesus monkeys
Dosage:	10 mg/kg
Administration:	Single, orally, 10 mg/kg
Result:	Possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days. Remained the plasma DPP-4 inhibition rates of 76.16% and 43.41%, respectively at the end of second week and third week after administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (214.39 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1439 mL	10.7197 mL	21.4394 mL
5 mM	0.4288 mL	2.1439 mL	4.2879 mL
10 mM	0.2144 mL	1.0720 mL	2.1439 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (2.68 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.68 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.68 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.68 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。