A competitive antagonist of nAChRs and non-depolarizing muscle relaxant
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Metabolite(s)
27170(S)-Laudanosine
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Cisatracurium (besylate)

Item No. 22959

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,1'R,2R,2'R)-2,2'-[1,5-pentanediylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-isoquinolinium, dibenzenesulfonate
CAS Number
96946-42-8
Molecular Formula
C53H72N2O12 • 2C6H5O3S
Formula Weight
1243.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
280 nm
SMILES
COC1=C(OC)C=C(C[C@@H]2C(C=C(OC)C(OC)=C3)=C3CC[N@+]2(C)CCC(OCCCCCOC(CC[N@@+]4(C)CCC(C=C(OC)C(OC)=C5)=C5[C@H]4CC6=CC(OC)=C(OC)C=C6)=O)=O)C=C1.[O-]S(C7=CC=CC=C7)(=O)=O.[O-]S(C8=CC=CC=C8)(=O)=O
InChi Code
InChI=1S/C53H72N2O12.2C6H6O3S/c1-54(22-18-38-32-48(62-7)50(64-9)34-40(38)42(54)28-36-14-16-44(58-3)46(30-36)60-5)24-20-52(56)66-26-12-11-13-27-67-53(57)21-25-55(2)23-19-39-33-49(63-8)51(65-10)35-41(39)43(55)29-37-15-17-45(59-4)47(31-37)61-6;2*7-10(8,9)6-4-2-1-3-5-6/h14-17,30-35,42-43H,11-13,18-29H2,1-10H3;2*1-5H,(H,7,8,9)/q+2;;/p-2/t42-,43-,54-,55-;;/m1../s1
InChi Key
XXZSQOVSEBAPGS-DONVQRBFSA-L
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $103

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    50 mg

    $194

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    100 mg

    $363

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    250 mg

    $801

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    Product Description

    Cisatracurium is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) and non-depolarizing muscle relaxant.1,2 It inhibits stimulation of human adult muscle nAChRs by acetylcholine (Item No. 23829) with an IC50 value of 10 nM.1 It also inhibits mouse nAChRs with IC50 values of 54 and 115 nM for adult and embryonic receptors, respectively.3 Cisatracurium increases apoptosis in HUVEC cells and decreases proliferation of HepG2 and HUVEC cells in vitro in a concentration-dependent manner.4,5 It reduces the magnitude of electrically-evoked twitch tensions in isolated rat extensor digitorum longus and soleus sciatic nerve muscle preparations in a dose-dependent manner.2 Cisatracurium blocks electrically-evoked muscle twitches in anesthetized rabbits with an ED95 value of 0.04 mg/kg.6 Formulations containing cisatracurium have been used to facilitate intubation prior to surgery and as muscle relaxants.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, M., and Dilger, J.P. Synergy between pairs of competitive antagonists at adult human muscle acetylcholine receptors. Anesth. Analg. 107(2), 525-533 (2008).

    2. Huang, L., Chen, D., and Li, S. Streptozotocin diabetes attenuates the effects of nondepolarizing neuromuscular relaxants on rat muscles. Korean J. Physiol. Pharmacol. 18(6), 461-467 (2014).

    3. Demazumder, D., and Dilger, J.P. The kinetics of competitive antagonism by cisatracurium of embryonic and adult nicotinic acetylcholine receptors. Mol. Pharmacol. 60(4), 797-807 (2001).

    4. Amann, A., Rieder, J., Fleischer, M., et al. The influence of atracurium, cisatracurium, and mivacurium on the proliferation of two human cell lines in vitro. Anesth. Analg. 93(3), 690-696 (2001).

    5. Zhuang, H., Tian, W., Li, W., et al. Autophagic cell death and apoptosis jointly mediate cisatracurium besylate-induced cell injury. Int. J. Mol. Sci. 17(4), 515 (2016).

    6. Diaz, L.L., Zhang, J., and Heerdt, P.M. Comparative pharmacodynamics of pancuronium, cisatracurium, and CW002 in rabbits. J. Am. Assoc. Lab. Anim. Sci. 53(3), 283-289 (2014).