1. GPCR/G Protein
  2. P2Y Receptor
  3. P2Y14R antagonist 2

P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis.

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P2Y14R antagonist 2 Chemical Structure

P2Y14R antagonist 2 Chemical Structure

CAS No. : 2989271-65-8

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Description

P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis[1].

IC50 & Target[1]

P2Y14 Receptor

0.40 nM (IC50)

In Vivo

P2Y14R antagonist 2 (50, 100 µM for 100µL per mice; rectally administered, daily for 7 days) shows anti-inflammatory activity in mice with colitis[1].
Pharmacokinetic Parameters[1].

Parameters dose (mg/kg) Cmax (ng/mL) T1/2 (min) Tmax (min) AUCall (min*ng/mL) CL (mL/min/kg) F (%)
iv 1.0 - 21 ± 8.4 - 27924 ± 5520 133.8 ± 33 -
po 5.0 518.25 ± 196.26 177.6 ± 24.6 15 90744 ± 21613 232.2 ± 46.2 65.0

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

Animal Model: 6-8 weeks, 20-22 g, male C57BL/6 mice (colitis) [1]
Dosage: 50, 100 µM for 100µL per mice
Administration: Rectally administered, daily for 7 days
Result: Alleviated DSS-induced body weight loss, loose stools, rectal bleeding, colon shortening, and elevated spleen weighted index.
Molecular Weight

372.37

Formula

C18H13FN2O4S

CAS No.
SMILES

O=C(C1=CC(NC(C2=CC=C(C=C2)C)=O)=C(S1)OC3=NC=C(C=C3)F)O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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P2Y14R antagonist 2 Related Classifications

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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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P2Y14R antagonist 2
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HY-162661
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