CHIKV-IN-2|cas:2361289-44-1|西域试剂

CHIKV-IN-2,98.15%

产品编号：Bellancom-132174| CAS NO：2361289-44-1| 分子式：C₂₃H₂₆N₂O₂| 分子量：362.46

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	价格	库存与货期
Bellancom-132174	￥3000.00	杭州北京（现货）
Bellancom-132174	￥4800.00	杭州北京（现货）
Bellancom-132174	￥9500.00	杭州北京（现货）
Bellancom-132174	￥14500.00	杭州北京（现货）
Bellancom-132174	￥22500.00	杭州北京（现货）

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CHIKV-IN-2

产品介绍

CHIKV-IN-2 是一种针对基孔肯雅病毒 (CHIKV) 的有效抑制剂，具有出色的细胞抗病毒活性 (EC₉₀=270 nM) 和改善的肝微粒体稳定性。CHIKV-IN-2 对细胞靶二氢乳清酸脱氢酶 (DHODH) 表现出抑制活性。

生物活性

CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC₉₀=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.

体外研究

CHIKV-IN-2 (compound 8q) is a potent pan-alphavirus inhibitor, with EC₉₀s of 0.85-2.5 μM for CHIKV clinical isolates and attenuated vaccine strains.
CHIKV-IN-2 is active against alphavirus VEEV (EC₉₀=0.40 μM) as well as flaviviruses such as West Nile Virus (WNV, EC₉₀=0.20 μM) and Dengue Virus Strain-2 (DENV-2, EC₉₀=0.60 μM).

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

体内研究

CHIKV-IN-2 (compound 8q) (80 mg/kg; i.p. twice a day for 3 days) significantly decreases infectious CHIKV dissemination to other tissues of mice.
CHIKV-IN-2 (40 mg/kg; p.o., i.p., s.c.) exhibits moderate bioavailability (F=41%, 43%, 4%), terminal elimination half-life (t_1/2=9.9, 18.5, 18.6 h) and C_max (642, 858, 90 ng/mL) in mice.
CHIKV-IN-2 (1 mg/kg; i.v.) exhibits terminal elimination half-life (t_1/2= 2.02 h) and AUC (497 h•ng/mL) in mice.

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

Animal Model:	Female and male C57BL/6 mice
Dosage:	80 mg/kg
Administration:	I.p. twice a day for 3 days
Result:	Failed to inhibit virus loads at the site of infection. Decreased virus dissemination to other tissues.

Animal Model:	Male C57BL/6 mice were challenged with CHIKV in the right footpad
Dosage:	1 mg/kg for i.v. and 40 mg/kg for p.o., i.p., s.c. (Pharmacokinetic Analysis)
Administration:	I.v., p.o., i.p., s.c.
Result:	I.v.: t_1/2= 2.02 h; AUC=497 h•ng/mL. P.o.: F=41%; t_1/2=9.9 h; C_max=642 ng/mL. I.p.: F=43%; t_1/2=18.5 h; C_max=858 ng/mL. S.c.: F=4%; t_1/2=18.6 h; C_max=90 ng/mL.

体内研究

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

Animal Model:	Female and male C57BL/6 mice
Dosage:	80 mg/kg
Administration:	I.p. twice a day for 3 days
Result:	Failed to inhibit virus loads at the site of infection. Decreased virus dissemination to other tissues.

Animal Model:	Male C57BL/6 mice were challenged with CHIKV in the right footpad
Dosage:	1 mg/kg for i.v. and 40 mg/kg for p.o., i.p., s.c. (Pharmacokinetic Analysis)
Administration:	I.v., p.o., i.p., s.c.
Result:	I.v.: t_1/2= 2.02 h; AUC=497 h•ng/mL. P.o.: F=41%; t_1/2=9.9 h; C_max=642 ng/mL. I.p.: F=43%; t_1/2=18.5 h; C_max=858 ng/mL. S.c.: F=4%; t_1/2=18.6 h; C_max=90 ng/mL.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (275.89 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7589 mL	13.7946 mL	27.5893 mL
5 mM	0.5518 mL	2.7589 mL	5.5179 mL
10 mM	0.2759 mL	1.3795 mL	2.7589 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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液。
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 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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.90 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。