Syrosingopine

Syrosingopine is an inhibitor of monocarboxylate transporter 1 (MCT1) and MCT4 (IC50s = 2,500 and 40 nM, respectively). It inhibits MCT-facilitated lactate export and decreases intracellular pH in HL-60 promyeloblast cells when used at a concentration of 10 µM. Syrosingopine (5 µM), in combination with metformin (Cay-13118), decreases cell growth in HL-60 cells. Intravenous administration of syrosingopine (0.5 mg/kg) reduces heart norepinephrine levels, mean arterial pressure (MAP), and pulse rate in normotensive dogs. Formulations containing syrosingopine have been used in the treatment of hypertension.Formal Name: (3beta,16beta,17alpha,18beta,20alpha)-18-[[4-[(ethoxycarbonyl)oxy]-3,5-dimethoxybenzoyl]oxy]-11,17-dimethoxy-yohimban-16-carboxylic acid, methyl ester. CAS Number: 84-36-6. Synonyms: NSC 77030, SU 3118. Molecular Formula: C35H42N2O11. Formula Weight: 666.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2 mg/ml, DMSO: Slightly soluble, PBS (pH 7.2): 0.3 mg/ml. lambdamax: 212 nm. SMILES: COC([C@H]1[C@@]2([H])C[C@]3([H])C4=C(CCN3C[C@@]2([H])C[C@H]([C@@H]1OC)OC(C5=CC(OC)=C(C(OC)=C5)OC(OCC)=O)=O)C6=CC=C(OC)C=C6N4)=O. InChi Code: InChI=1S/C35H42N2O11/c1-7-46-35(40)48-31-26(42-3)12-18(13-27(31)43-4)33(38)47-28-14-19-17-37-11-10-22-21-9-8-20(41-2)15-24(21)36-30(22)25(37)16-23(19)29(32(28)44-5)34(39)45-6/h8-9,12-13,15,19,23,25,28-29,32,36H,7,10-11,14,16-17H2,1-6H3/t19-,23+,25-,28-,29+,32+/m1/s1. InChi Key: ZCDNRPPFBQDQHR-SSYATKPKSA-N.