HIF-PHD-IN-1|cas:1567657-46-8|西域试剂

HIF-PHD-IN-1,99.37%

产品编号：Bellancom-131346| CAS NO：1567657-46-8| 分子式：C₁₇H₁₂Cl₂N₆O₃| 分子量：419.22

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-131346		￥5800.00	杭州北京（现货）
Bellancom-131346		￥10500.00	杭州北京（现货）

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HIF-PHD-IN-1

产品介绍

HIF-PHD-IN-1 是一种具有口服活性的缺氧诱导因子脯氨酰羟化酶结构域 (HIF-PHD) 的抑制剂，抑制 hHIF-PHD2 的 IC₅₀ 值为 54 nM。HIF-PHD-IN-1 是有希望的肾性贫血研究活性分子。

生物活性

HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC₅₀ of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia.

体外研究

体内研究

HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats.
HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats.
HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats.

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

Animal Model:	Male SD Rats excising ﬁve-sixths of their kidneys
Dosage:	0.5, 1, 2 mg/kg
Administration:	P.o. once daily for 4 weeks
Result:	Improved blood hemoglobin levels starting at weeks 2 and 1 in the groups receiving 1 and 2 (mg/kg)/day, respectively.

Animal Model:	Male SD Rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	Single p.o. or i.v.
Result:	C_max=1839 ng/mL (p.o.); C_max=12357ng/mL (i.v.); F=77%.

体内研究

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

Animal Model:	Male SD Rats excising ﬁve-sixths of their kidneys
Dosage:	0.5, 1, 2 mg/kg
Administration:	P.o. once daily for 4 weeks
Result:	Improved blood hemoglobin levels starting at weeks 2 and 1 in the groups receiving 1 and 2 (mg/kg)/day, respectively.

Animal Model:	Male SD Rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	Single p.o. or i.v.
Result:	C_max=1839 ng/mL (p.o.); C_max=12357ng/mL (i.v.); F=77%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (238.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3854 mL	11.9269 mL	23.8538 mL
5 mM	0.4771 mL	2.3854 mL	4.7708 mL
10 mM	0.2385 mL	1.1927 mL	2.3854 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 (sealed storage, away from moisture and light)。-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% corn oil
Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.96 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。