{"product_id":"m19817","title":"SB-616234-A","description":"\u003cp style=\"padding-left: 1em;\"\u003eSB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 908601-49-0\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 574.11\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C32H36ClN5O3\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 6-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-5-methoxy-1-[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carbonyl]-2,3-dihydro-1H-indole hydrochloride\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e Cl.COC1=CC2CCN(C(=O)C3C=CC(=CC=3)C3=CC=C(C=C3C)C3=NOC(C)=N3)C=2C=C1N1C[C@H](C)N[C@H](C)C1\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e VPWVEPYFVFBHQR-XKFLBXONSA-N\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C32H35N5O3.ClH\/c1-19-14-26(31-34-22(4)40-35-31)10-11-27(19)23-6-8-24(9-7-23)32(38)37-13-12-25-15-30(39-5)29(16-28(25)37)36-17-20(2)33-21(3)18-36;\/h6-11,14-16,20-21,33H,12-13,17-18H2,1-5H3;1H\/t20-,21+;\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e DMSO : 10 mg\/mL (17.42 mM; Need ultrasonic).\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eSB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2\/S1 ratios of 1.8 and 1.6, respectively).\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eSB-616234-A reverses the 5-HT1\/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg\/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg\/kg i.p., respectively. SB-616234-A (0.3-30 mg\/kg p.o.) causes a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED50 of 2.83 ± 0.39 mg\/kg p.o.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M19817-C \/ Contact sales@xcessbio.com for quotation","offer_id":39524030873739,"sku":"0","price":100.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/files\/1686560915341.png?v=1686560942","url":"https:\/\/www.xcessbio.com\/products\/m19817","provider":"Xcess Biosciences","version":"1.0","type":"link"}