GPR

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  1. CRTH2 antagonist

    OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist.
  2. CRTH2 receptor antagonist

    AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM.
  3. GPR139 antagonist

    NCRW0005-F05, first antagonist selective for GPR139 (IC50 value 0.21 uM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054.
  4. EBI2 (GPR183) antagonist

    ML401 is an antagonist of the EBI2 receptor with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity.
  5. GPR171 antagonist

    MS21570 is a selective GPR171 antagonist, with an IC50 of 220 nM.
  6. GPR55 antagonist

    ML191 (CCG-152883, CID-23612552) is an antagonist of GPR55 with EC50 of 1.076 ?M in U2OS cells overexpressing GPR55.
  7. GPR55 antagonist

    ML 193 is a selective GPR55 antagonist (IC50 = 221 nM). Exhibits >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively. Inhibits ERK signaling in vitro.

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