1. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel
  2. FAAH Potassium Channel
  3. SRP-001

SRP-001 是一种具备口服活性与血脑屏障穿透能力的镇痛和解热剂。SRP-001 可降低 FAAH 的表达水平,轻度抑制 hERG 电流,生成 AM404 (HY-101388),维持肝紧密连接的完整性。SRP-001 具有镇痛、解热、抗伤害感受作用。

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SRP-001

SRP-001 Chemical Structure

CAS No. : 2290606-49-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects[1].

体外研究
(In Vitro)

SRP-001 (100 μM) 可微弱抑制胚肾细胞中的 hERG 电流,100 μM 浓度下可使电流降低 21.4%[1]
SRP-001 (100-5000 μg per plate) 无论是否经过代谢活化,均不会在鼠伤寒沙门氏菌或大肠杆菌 WP2 uvrA 菌株中诱导回复突变,且在 Ames 试验中无致突变性[1]

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

体内研究
(In Vivo)

SRP-001 (32-100 mg/kg;口服;累计给予间隔 60 分钟) 可在 CFA 诱导炎症痛的幼年雄性 Sprague-Dawley 大鼠中产生剂量依赖性镇痛作用,提高其对机械和热刺激的缩爪阈值[1]
SRP-001 (32-100 mg/kg;口服) 可在完全弗氏佐剂 (CFA) 诱导炎症疼痛的老年雄性 Sprague-Dawley 大鼠中产生镇痛作用,其效力与等效剂量的对乙酰氨基酚 (ApAP) 相当[1]
SRP-001 (32-100 mg/kg;口服;单次) 可在幼龄及雄性老年小鼠、雌性幼龄小鼠的内脏疼痛模型中产生剂量依赖性镇痛作用[1]
SRP-001 (75 mg/kg;口服;单次) 可在酵母诱导发热的雄性 CD1 小鼠中产生解热活性,其降低核心体温的效果与 75 mg/kg 的 ApAP 相似[1]
SRP-001 (32 mg/kg;腹腔注射;单次) 在 Sprague-Dawley 大鼠中脑导水管周围灰质 (PAG) 中产生的镇痛代谢物 AM404 水平高于 32 mg/kg 剂量的 ApAP,这为其抗伤害感受作用机制提供了支持[1]

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

Animal Model: Sprague-Dawley (male, 2 months)[1]
Dosage: 32 mg/kg, 100 mg/kg
Administration: p.o.; cumulative doses 60 minutes apart
Result: Increased paw withdrawal threshold from 18 g to 40 g (32 mg/kg) and 55 g (100 mg/kg) in eVF testing for CFA-injected left hind paw.
Demonstrated comparable or greater antinociceptive efficacy than ApAP at equivalent doses.
Produced significant analgesia in the Hargreaves thermal sensitivity assay at 100 mg/kg.
分子量

405.47

Formula

C19H23N3O5S

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

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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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SRP-001
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HY-182589
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