1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Safotibant

Safotibant  (Synonyms: LF22-0542)

目录号: HY-100827
产品使用指南

Safotibant (LF22-0542) 是激肽 B1 受体 (BKB1R) 的选择性拮抗剂,对人源和鼠源 BKB1R 的 Ki 分别为 0.35 和 6.5 nM。Safotibant 在小鼠模型中表现出镇痛和抗炎活性。

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Safotibant Chemical Structure

Safotibant Chemical Structure

CAS No. : 633698-99-4

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查看 Bradykinin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model[1][2].

体内研究
(In Vivo)

Safotibant (10 mg/kg,皮下注射,每天 3 次,持续 8 天) 在 C3H/HeJ 小鼠溶骨性肉瘤异种移植模型中,对骨癌引发的疼痛具有镇痛活性,且不影响疾病进程[1]
Safotibant (一滴滴眼液,每天两次,持续 7 天) 在 streptozotocin (STZ) 诱导的大鼠糖尿病模型中,抑制炎症介质 B1R、iNOS、IL-1β、COX-2、VEGF-R2 和 HIF-1α 的表达,减轻糖尿病引发的视网膜炎症和氧化应激反应[2]

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

Animal Model: Osteolytic sarcoma xenograft C3H/HeJ mice model[1]
Dosage: 10 mg/kg
Administration: s.c., 3 times a day for 8 days
Result: Decreased numbers of flinching and time spent on spontaneous guarding.
Animal Model: Streptozotocin (STZ)-diabetic Wistar rats model[2]
Dosage: One eye drop
Administration: On eyes application, twice a day for 7 days
Result: Reversed retinal vascular hyperpermeability, decreased levels of retinal leukostasis and superoxide anion in 3 retinal nuclear layers.
分子量

502.63

Formula

C25H34N4O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Safotibant
目录号:
HY-100827
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