A selective AT2 receptor antagonist
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EMA401

Item No. 22988

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S)-2-(2,2-diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinolinecarboxylic acid
CAS Number
1316755-16-4
Molecular Formula
C32H29NO5
Formula Weight
507.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 0.1 mg/ml
SMILES
O=C(N1[C@H](C(O)=O)CC(C(OCC2=CC=CC=C2)=C(OC)C=C3)=C3C1)C(C4=CC=CC=C4)C5=CC=CC=C5
InChi Code
InChI=1S/C32H29NO5/c1-37-28-18-17-25-20-33(31(34)29(23-13-7-3-8-14-23)24-15-9-4-10-16-24)27(32(35)36)19-26(25)30(28)38-21-22-11-5-2-6-12-22/h2-18,27,29H,19-21H2,1H3,(H,35,36)/t27-/m0/s1
InChi Key
GHBCIXGRCZIPNQ-MHZLTWQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $62

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    5 mg

    $164

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    10 mg

    $295

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    25 mg

    $589

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    Product Description

    EMA401 is an orally bioavailable and selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively).1 It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures.2 EMA401 has analgesic effects in a rat model of neuropathic pain induced by chronic constriction injury.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, M.T., Wyse, B.D., and Edwards, S.R. Small molecule angiotensin II type 2 receptor (AT₂R) antagonists as novel analgesics for neuropathic pain: Comparative pharmacokinetics, radioligand binding, and efficacy in rats. Pain Med. 14(5), 692-705 (2013).

    2. Anand, U., Facer, P., Yiangou, Y., et al. Angiotensin II type 2 receptor (AT2R) localization and antagonist-mediated inhibition of capsaicin responses and neurite outgrowth in human and rat sensory neurons. Eur J. Pain. 17(7), 1012-1026 (2012).

    3. Hanyan, X., Benzhuo, Z., Liping, H., et al. Analgesic effect of angiotensin angiotensin Ⅱ type 2 receptor antagonist EMA401 on neuropathic pain in rats and its mechanism. Chin. J. Pathophysiol. 33(1), 110-115 (2017).