A 5-HT5A antagonist
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SB-699551 (hydrochloride)

Item No. 42517

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-cyclopentyl-N-(2-(dimethylamino)ethyl)-N-((4'-((phenethylamino)methyl)-[1,1'-biphenyl]-4-yl)methyl)propanamide, hydrochloride
Molecular Formula
C34H45N3O • XHCl
Formula Weight
511.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Soluble: ≥10 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(CCC1CCCC1)N(CCN(C)C)CC2=CC=C(C3=CC=C(CNCCC4=CC=CC=C4)C=C3)C=C2.Cl
InChi Code
InChI=1S/C34H45N3O.ClH/c1-36(2)24-25-37(34(38)21-16-28-10-6-7-11-28)27-31-14-19-33(20-15-31)32-17-12-30(13-18-32)26-35-23-22-29-8-4-3-5-9-29;/h3-5,8-9,12-15,17-20,28,35H,6-7,10-11,16,21-27H2,1-2H3;1H
InChi Key
GOKSGMDKZDVEEZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    5 mg

    $138

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    10 mg

    $220

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    25 mg

    $482

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    50 mg

    $825

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    Cayman Chemical
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    Product Description

    SB-699551 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT5A (Ki = 6.31 nM).1 It is selective for 5-HT5A over a panel of 14 other receptors (Kis = >315 nM for all) but does inhibit the serotonin transporter (SERT; Ki = 25.12 nM). SB-699551 also decreases sphere formation in patient-derived xenograft (PDX) breast cancer cells (IC50 = 596 nM).2 It decreases tumor volume in combination with docetaxel (Item No. 11637) in a PDX mouse model of breast cancer. SB-699551 inhibits cued fear conditioning in mice (ED50 = 25.4 mg/kg).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Corbett, D.F., Heightman, T.D., Moss, S.F., et al. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg. Med. Chem. Lett. 15(18), 4014-4018 (2005).

    2. Gwynne, W.D., Shakeel, M.S., Girgis-Gabardo, A., et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer 20(1), 724 (2020).

    3. Kassai, F., Schlumberger, C., Kedves, R., et al. Effect of 5-HT5A antagonists in animal models of schizophrenia, anxiety and depression. Behav. Pharmacol. 23(4), 397-406 (2012).