TC-SP 14
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.
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- CAS No.: 1257093-40-5
- Formule: C25H20F2N2O2S
- Masse moléculaire:450.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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S1PR1 0.042 μM (EC50) |
S1PR3 3.47 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
3.47 μM
Compound: 14
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Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay
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[PMID: 24900287] |
| U2OS | EC50 |
0.042 μM
Compound: 14
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Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization after 1 hr
Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization after 1 hr
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[PMID: 24900287] |
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats (female, n = 5/group)[1]
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Dosage:0.3, 1.0, and 3.0 mg/kg
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Administration:Orally, once
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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).
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Animal Model:OVA-immunized Lewis rats (female, n = 8/group)[1]
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Dosage:0.1, 0.3, 1.0, and 3.0 mg/kg
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Administration:Orally, daily for 10 days
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Result:Significant reduced OVA-induced ear swelling at doses of 0.3 mg/kg and higher.
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Animal Model:Female Sprague-Dawley rats, Male Cynomolgus (NHP (nonhuman primates)) (n=3/group)[1]
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Dosage:2 (IV, rat), 4 (IV, NHP), 10 (PO, NHP), 15 mg/kg (PO, rat)
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Administration:IV, PO, once (Pharmacokinetic Analysis)
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Result:Possessed acceptable characteristics, demonstrated low clearance, moderate steady state volumes of distribution, moderate-to-long mean residence times, and acceptable oral bioavailability.
Chemical Information
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CAS No. 1257093-40-5
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Masse moléculaire 450.50
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Formule C25H20F2N2O2S
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SMILES
O=C(C1CN(CC2=CC=C(C3=NC4=CC(CC5=CC=CC=C5F)=CC=C4S3)C(F)=C2)C1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-SP 14 Related Classifications
HY-108492 Related Classifications
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