Biochem/physiol Actions
Selective relaxant binding agent (SRBA) for complexing aminosteroid nondepolarizing neuromuscular blockers (NMBs) in vitro and in vivo.
Sugammadex (Org 25969) is a selective relaxant binding agent (SRBA) for complexing aminosteroid nonpolarizing neuromuscular blockers (NMBs), including pipecuronium, rocuronium and vecuronium. Sugammadex effectively recovers muscle twitch blockade in vitro (EC50 = 1.2 μM, Emax = 95.1%; isolated mouse hemi-diaphragm under 90% block by 3.6 μM rocuronium) and reverses neuromuscular blockade in vivo (ED50 = 30 nmol/kg i.v. & Emax = 92.5% with guinea pigs under 90% neuromuscular block by 10 nmol/kg/min rocuronium i.v. infusion; >90% recovery at 1 mg/kg or 0.46 μmol/kg i.v. of M. tibialis contractions of cats under 95% block by 10.24 nmol/kg/min rocuronium i.v. infusion).
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | O[C@@H]1[C@@H](O)[C@@H](O[C@@H]2[C@@H](CSCCC(O[Na])=O)O[C@H](O[C@@H]3[C@@H](CSCCC(O[Na])=O)O[C@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@@H]5[C@@H](CSCCC(O[Na])=O)O[C@H](O[C@@H]6[C@@H](CSCCC(O[Na])=O)O[C@H]7[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)O[C@@H]4CSCCC(O[Na]) |
| InChI | 1S/C72H112O48S8.8Na/c73-33(74)1-9-121-17-25-57-41(89)49(97)65(105-25)114-58-26(18-122-10-2-34(75)76)107-67(51(99)43(58)91)116-60-28(20-124-12-4-36(79)80)109-69(53(101)45(60)93)118-62-30(22-126-14-6-38(83)84)111-71(55(103)47(62)95)120-64-32(24-128-16-8-40(87)88)112-72(56(104)48(64)96)119-63-31(23-127-15-7-39(85)86)110-70(54(102)46(63)94)117-61-29(21-125-13-5-37(81)82)108-68(52(100)44(61)92)115-59-27(19-123-11-3-35(77)78)106-66(113-57)50(98)42(59)90;;;;;;;;/h25-32,41-72,89-104H,1-24H2,(H,73,74)(H,75,76)(H,77,78)(H,79,80)(H,81,82)(H,83,84)(H,85,86)(H,87,88);;;;;;;;/q;8*+1/p-8/t25-,26-,27-,28-,29-,30-,31-,32-,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-;;;;;;;;/m1......../s1 |
| InChI key | KMGKABOMYQLLDJ-VKHHSAQNSA-F |

