2. GPCR/G Protein
  3. LPL Receptor
  4. TC-SP 14

TC-SP 14 (compound 14) 是一种口服有效的 S1P1 激动剂 (EC50 = 0.042 μM)，在 S1P3 处活性极低 (EC50 = 3.47 μM)。TC-SP 14 可显著降低血液淋巴细胞计数，减弱对抗原挑战的迟发型超敏反应(DTH)。

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TC-SP 14 Chemical Structure

TC-SP 14 Chemical Structure

CAS No. : 1257093-40-5

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TC-SP 14 相关抗体

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查看 LPL Receptor 亚型特异性产品:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge[1].

IC50 & Target

S1PR1

0.042 μM (EC50)

S1PR3

3.47 μM (EC50)

体外研究
(In Vitro)

TC-SP 14 (compound 14) neither inhibits nor induces human cytochrome P450 enzymes, is nonmutagenic, and dose not significantly inhibit the hERG channel[1].

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

TC-SP 14 相关抗体:
体内研究
(In Vivo)

TC-SP 14 (compound 14) (0-3 mg/kg, Orally, once) produces a dose-dependent reduction in circulating blood lymphocytes 24 h postdose[1].
TC-SP 14 (0-3 mg/kg, Orally, daily for 10 days) significant reduces ovalbumin (OVA)-induced ear swelling[1].
TC-SP 14 (2-15 mg/kg, IV or PO, once) possesses acceptable characteristics[1].
Pharmacokinetic Parameters of TC-SP 14 in female Sprague-Dawley rats and male Cynomolgus [1].

species rat NHP
CL (L/h/kg) 0.33 0.50
Vss (L/kg) 3.3 1.6
T1/2 (h) 7.5 35.2
MRT (h) 10 3.3
% F 68 23

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

Animal Model: Lewis rats (female, n = 5/group)[1]
Dosage: 0.3, 1.0, and 3.0 mg/kg
Administration: Orally, once
Result: Produced a dose-dependent reduction in circulating blood lymphocytes 24 h postdose, resulted in near maximal lymphopenia at 3.0 mg/kg (74% reduction in lymphocytes vs vehicle).
Animal Model: OVA-immunized Lewis rats (female, n = 8/group)[1]
Dosage: 0.1, 0.3, 1.0, and 3.0 mg/kg
Administration: Orally, daily for 10 days
Result: Significant reduced OVA-induced ear swelling at doses of 0.3 mg/kg and higher.
Animal Model: Female Sprague-Dawley rats, Male Cynomolgus (NHP (nonhuman primates)) (n=3/group)[1]
Dosage: 2 (IV, rat), 4 (IV, NHP), 10 (PO, NHP), 15 mg/kg (PO, rat)
Administration: IV, PO, once (Pharmacokinetic Analysis)
Result: Possessed acceptable characteristics, demonstrated low clearance, moderate steady state volumes of distribution, moderate-to-long mean residence times, and acceptable oral bioavailability.
分子量

450.50

Formula

C25H20F2N2O2S
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

TC-SP 14 相关分类

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  • 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.

Keywords:

TC-SP 141257093-40-5LPL ReceptorLysophospholipid ReceptorLymphocytesOrally activeInflammationInhibitorinhibitorinhibit

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产品名称：
TC-SP 14
目录号：
HY-108492
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