Terlipressin (acetate)

Terlipressin is a prodrug form of the vasopressin peptide lysipressin and a partial agonist of the vasopressin V1A receptor (Ki = 0.85 µM). It is also an agonist of vasopressin V1B and V2 receptors (Kis = 1.11 and 1.58 µM, respectively). It increases mean arterial pressure (MAP) and decreases mortality in a rat model of uncontrolled hemorrhagic shock when administered at a dose of 15 µg/kg. Terlipressin (2.6 µg/kg per hour), in combination with norepinephrine, improves vascular reactivity and increases survival time in a rat model of cecal ligation and puncture-induced septic shock and a rabbit model of LPS-induced septic shock. It also increases MAP in a rat model of liver cirrhosis with portal hypertension, arterial hypotension, high cardiac output, and low systemic vascular resistance.Formal Name: N-(glycylglycylglycyl)-8-L-lysine-vasopressin, acetate. CAS Number: 914453-96-6. Synonyms: Glycylpressin, Remestyp. Molecular Formula: C52H74N16O15S2 . XC2H4O2. Formula Weight: 1227.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: Partially soluble, PBS (pH 7.2): 10 mg/ml. SMILES: OC(C=C1)=CC=C1C[C@H](NC([C@@H](NC(CNC(CNC(CN)=O)=O)=O)CSSC[C@@H](C(N2CCC[C@H]2C(N[C@@H](CCCCN)C(NCC(N)=O)=O)=O)=O)NC([C@H](CC(N)=O)N3)=O)=O)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CCC(N)=O)C3=O)=O)=O.CC(O)=O. InChi Code: InChI=1S/C52H74N16O15S2.C2H4O2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37,1-2(3)4/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80),1H3,(H,3,4)/t31-,32-,33-,34-,35-,36-,37-,38-,/m0./s1. InChi Key: BYDVFOPTAIPAGA-LCGYVTRFSA-N.