(R)-BPO-27|cas:1415390-47-4|西域试剂

(R)-BPO-27,99.86%

产品编号：Bellancom-19778| CAS NO：1415390-47-4| 分子式：C₂₆H₁₈BrN₃O₆| 分子量：548.34

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-19778	￥1500.00	杭州北京（现货）
Bellancom-19778	￥3500.00	杭州北京（现货）
Bellancom-19778	￥5000.00	杭州北京（现货）
Bellancom-19778	￥15000.00	杭州北京（现货）
Bellancom-19778	￥21000.00	杭州北京（现货）

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(R)-BPO-27

产品介绍

(R)-BPO-27 是 BPO-27 的 R 型对映体，是一种有效的、具有口服活性的、ATP 竞争性的 CFTR 抑制剂，具有 IC₅₀ 的 4 nM。

生物活性

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC₅₀ of 4 nM.

体外研究

(R)-BPO-27 exhibits a dose-response inhibition and inhibits the CFTR current by 50% at 0.53 nM in HEK-293T cells. (R)-BPO-27 acts from the cytoplasmic side and has low membrane permeability.
(R)-BPO-27 reduces the channel open probability (NPo) from 0.29 to 0.08, modestly reduces in mean channel open time, and strongly increases mean channel closed time in HEK-293T cells expressing human wild-type CFT in a single-channel patch-clamp experiment. Meanwhile, (S)-BPO-27 does not affect any of these parameters.
(R)-BPO-27 is applied directly to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC₅₀ of 600 pM in Single-channel electrophysiology assay.
(R)-BPO-27 (10 μM, 10 min pretreatment) inhibits Cl^- current with apparent IC₅₀ values of 5 and 10 nM for CPT-cAMP and 8-Br-cGMP, respectively, in CFTR-expressing FRT cells after CFTR stimulation by cAMP agonist. the IC₅₀ of 4 nM for inhibition of forskolin-stimulated CFTR Cl^- current in FRT cells.

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

体内研究

(R)-BPO-27 (interperitoneal administration; 10 mg/kg) decays with t_1/2≈1.6 h and gives sustained therapeutic concentrations in kidney in a PK study.
(R)-BPO-27 (intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery) prevents fluid accumulation in closed midjejunal loops produced by cholera toxin, giving an intestinal loop weight/length ratio similar to that in PBS-injected loops. This effect is dose-dependently and the IC₅₀ value is 0.1 mg/kg.
(R)-BPO-27 (intraperitoneal injection or oral administration; 5 mg/kg) shows a slow (R)-BPO-27 metabolism and produces sustained serum (R)-BPO-27 levels for at least 4 h. The AUC analysis gave an oral bioavailability of ∼94% for (R)-BPO-27 in mouse pharmacokinetics and toxicity study.

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

Animal Model:	Female CD1 mice (age 8–10 wk)
Dosage:	0.05, 0.15, 0.5, 1.5, and 5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery
Result:	Exhibited apparent efficacy in mice models of cholera and traveler’s diarrhea.

体内研究

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

Animal Model:	Female CD1 mice (age 8–10 wk)
Dosage:	0.05, 0.15, 0.5, 1.5, and 5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery
Result:	Exhibited apparent efficacy in mice models of cholera and traveler’s diarrhea.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 14.28 mg/mL (26.04 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8237 mL	9.1184 mL	18.2369 mL
5 mM	0.3647 mL	1.8237 mL	3.6474 mL
10 mM	0.1824 mL	0.9118 mL	1.8237 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式