TC-SP 14

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TC-SP 14

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1257093-40-5

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)。

生物活性

TC-SP 14 (compound 14) is an orally active and potentS1P1agonist (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].

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
T_1/2(h)	7.5	35.2
MRT (h)	10	3.3
% F	68	23

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

1257093-40-5

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.