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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC12185 Vabicaserin hydrochloride (SCA 136) Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
DCAPI1452 Valsartan Valsartan is a nonpeptide angiotensin II AT1-receptor antagonist with an IC50 ranging from 39.5 to 116 μM. This in turn causes blood vessel dilation.
DC11168 VCE-004.3 VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61).
DC7336 Vicriviroc maleate(Sch-417690) Featured Vicriviroc Malate is a potent CKR-5 (CCR5) antagonist with IC50 of 0.91 nM.
DC8814 Vipadenant Featured Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).
DC8613 Vortioxetine (Lu AA21004) Featured Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
DC8288 Vortioxetine hydrobromide Featured Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
DC12159 VU 0238429 Featured VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
DC9928 VU 0364770 Featured VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
DC12165 VU 0365114 Featured VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
DC9497 VU0152100 Featured VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
DC9255 VU0357017 Featured VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
DC11121 VU0418506 VU0418506 (VU 0418506) is a potent and selective mGlu4 positive allosteric modulator (PAM) with EC50 of 68 nM (hmGlu4).
DC11112 VU0453595 VU0453595 (VU453595) is a potent, selective M1 positive allosteric modulator (PAM) with EC50 of 3.2 uM (rM1).
DC11123 VU0467154 VU0467154 (VU 0467154) is a potent, selective M4 mAChR positive allosteric modulator with EC50 of 17.7 nM.
DC11437 VU0652957 Featured VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours).
DC11120 VU6004256 VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM).
DC10717 VU6005649 Featured VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.
DC10136 VUF10460 Featured VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
DC8851 VUF11207 Featured VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.
DC9668 WAY181187.HCl(WAY-181,187) Featured WAY-181187 is a potent and selective 5-HT6 receptor agonist. WAY-181187 possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (WAY-181187: EC50=6.6 nM, Emax=93%).
DC2050 WIN-55212-2 mesylate Featured WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
DC7341 WZ 811 Featured WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.
DC9498 Xanomeline (oxalate) Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist.
DC11248 XL-001 XL-001 (XL001) is a novel specific CB2 inverse agonist with Ki of 0.5 nM.
DC9007 Xylazine hydrochloride Xylazine Hydrochloride is α2 class of adrenergic receptor agonist.
DC9932 YL-0919 Featured YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.
DCAPI1015 Zafirlukast(Accolate) Zafirlukast(Accolate)
DC9435 Zibotentan(ZD4054) Featured Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
DCAPI1039 Ziprasidone HCl Ziprasidone HCl

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