A neurotensin receptor antagonist
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SR 142948 (hydrochloride)

Item No. 23911

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid, dihydrochloride
Molecular Formula
C39H51N5O6 • 2HCl
Formula Weight
758.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 0.1 mg/ml
λmax
202, 231 nm
SMILES
CN(CCCN(C)C(C1=CC=C(N2N=C(C(N[C@]3(C(O)=O)[C@H](C4)C[C@H]5C[C@@H]3C[C@@H]4C5)=O)C=C2C6=C(OC)C=CC=C6OC)C(C(C)C)=C1)=O)C.Cl.Cl
InChi Code
InChI=1S/C39H51N5O6.2ClH/c1-23(2)29-21-26(37(46)43(5)15-9-14-42(3)4)12-13-31(29)44-32(35-33(49-6)10-8-11-34(35)50-7)22-30(41-44)36(45)40-39(38(47)48)27-17-24-16-25(19-27)20-28(39)18-24;;/h8,10-13,21-25,27-28H,9,14-20H2,1-7H3,(H,40,45)(H,47,48);2*1H/t24-,25+,27-,28+,39-;;
InChi Key
AQJKZKHTPLUIAD-HAAOKSBBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $103

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    5 mg

    $236

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    10 mg

    $336

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    Product Description

    SR 142948 is an orally bioavailable non-peptide antagonist of neurotensin receptors (NTS; IC50s = 1.19, 0.32, and 3.96 nM for human recombinant NTS receptors expressed in CHO cells, HT-29 cells, and adult rat brain membranes, respectively).1 It inhibits inositol phosphate formation in HT-29 cells (IC50 = 3.9 nM) and intracellular calcium accumulation in CHO cells expressing human NTS receptors. SR 142948 (1 mg/kg, i.v.) inhibits the firing rate of rat ventral pallidum neurons with a longer duration of action than the NTS receptor antagonist SR 48692 (Item No. 20124).2 It also inhibits neurotensin-induced behavioral responses, including inhibition of neurotensin-induced turning behavior in mice when administered at doses ranging from 40 to 640 mg/kg and hypothermia and analgesia in rats and mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gully, D., Labeeuw, B., Boigegrain, R., et al. Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J. Pharmacol. Exp. Ther. 280(2), 802-812 (1997).

    2. Michaud, J.-C., Gueudet, C., and Soubrié, P. Effects of neurotensin receptor antagonists on the firing rate of rat ventral pallidum neurons. Neuroreport 11(7), 1437-1441 (2000).