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Endocrinology

Chemical structure

Cat.No.

Product Name

CAS no.

Target

  • YN440103 GSK1904529A 1089283-49-7

    GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM in cell-free assays, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

  • YN320148 IT1t dihydrochloride 1092776-63-0

    IT1t dihydrochloride is a potentCXCR4antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1nM.

  • YN320474 BI-671800 1093108-50-9

    BI-671800 (AP-761, Cmpd A) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to human CRTH2 and...

  • YN320872 JNJ-31020028 1094873-14-9

    JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.

  • YN320186 CCX140 1100318-47-5

    CCX140 (CCX140-B) is a potentCCR2antagonist.

  • YN321048 Aprocitentan 1103522-45-7

    Aprocitentan (ACT-132577) is the major  and  pharmacologically active metabolite of Macitentan. Aprocitentan is dualETA/ETBantagonist with IC50s of 3.4nM  and  987nM,  and pA2valus of 6.7  a...

  • YN320925 Bavisant dihydrochloride hydr... 1103522-80-0

    Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for A...

  • YN320738 MK-4256 1104599-69-0

    MK-4256 is a potent and selectiveSSTR3antagonist with IC50s of 0.66nM and 0.36nM in human and mouse receptor binding assays, respectively.

  • YN320419 SNT-207858 free base 1104662-66-9

    SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally activemelanocortin-4(MC-4)receptorantagonist. SNT207858 free base has an IC50 of 22nM (binding) and 11nM (function) on the MC-4 recepto...

  • YN440240 GSK1838705A 1116235-97-2

    GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.

  • YN321388 Doxazosin D8 1126848-44-9

    Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors.

  • YN481679 BRD7552 1137359-47-7

    BRD7552, a potentPDX1transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. B...

  • YN320380 TM-N1324 1144477-35-9

    TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9nM/5nM in the presence of Zn2+, and 280nM/180nM in the absence of Zn2+forhuman/murine GPR39.

  • YN481784 Methimazole D3 1160932-07-9

    Methimazole D3 is a deuterium labeled Methimazole. Methimazole is an antithyroid drug used for the treatment of the hyperthyroidism in humans and animals.

  • YN321201 TG4-155 1164462-05-8

    TG4-155 is a potent, brain-permeant and selectiveEP2 receptorantagonist with a Ki of 9.9nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. TG4-155 has an EP2 Schild KBof 2.4nM and display...

  • YN480331 ML 145 1164500-72-4

    ML 145 is a selectiveGPR35/CXCR8antagonist with anIC50/EC50of 20.1nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic ta...

  • YN481378 Ligandrol 1165910-22-4

    Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.

  • YN321341 Doxylamine D5 1173020-59-1

    Doxylamine D5 is deuterium labeled Doxylamine.

  • YN320074 Clenproperol-D7 1173021-09-4

    Clenproperol-D7 is the deuterium labeled Clenproperol. Clenproperol is a β2-adrenergic agonist.

  • YN321188 RS102895 hydrochloride 1173022-16-6

    RS102895 hydrochloride is a potentCCR2antagonist, with an IC50 of 360nM, and shows no effect on CCR1.

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