An NK3 receptor antagonist
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SB 222200

Item No. 29422

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide
CAS Number
174635-69-9
Molecular Formula
C26H24N2O
Formula Weight
380.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 10mg/mLEthanol: 15mg/mLEthanol:PBS (pH 7.2) (1:2): 0.3mg/mL
λmax
232 nm
SMILES
CC[C@H](NC(C1=C(C)C(C2=CC=CC=C2)=NC3=C1C=CC=C3)=O)C4=CC=CC=C4
InChi Code
InChI=1S/C26H24N2O/c1-3-22(19-12-6-4-7-13-19)28-26(29)24-18(2)25(20-14-8-5-9-15-20)27-23-17-11-10-16-21(23)24/h4-17,22H,3H2,1-2H3,(H,28,29)/t22-/m0/s1
InChi Key
MQNYRKWJSMQECI-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $129

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    10 mg

    $245

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    25 mg

    $574

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    50 mg

    $1,016

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    Product Description

    SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).1 It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.2 It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sarau, H.M., Griswold, D.E., Bush, B., et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J. Pharmacol. Exp. Ther. 295(1), 373-381 (2000).

    2. Lessard, A., Laurin, M., Yamaguchi, N., et al. Central anti-hypertensive effect of tachykinin NK3 receptor antagonists in rat. Eur. J. Pharmacol. 486(1), 75-83 (2004).