A 5-HT2B receptor antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

RS 127445 (hydrochloride)

Item No. 23451

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine, monohydrochloride
CAS Number
199864-86-3
Molecular Formula
C17H16FN3 • HCl
Formula Weight
317.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
223, 309 nm
SMILES
FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=C1C=CC=C3.Cl
InChi Code
InChI=1S/C17H16FN3.ClH/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13;/h3-10H,1-2H3,(H2,19,20,21);1H
InChi Key
MKJPYBJBPRFMHL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

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.

Download most recent Certificate of Analysis for this product

    1 mg

    $36

    Add

    5 mg

    $120

    Add

    10 mg

    $219

    Add
    Product Description

    RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM).1 It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT (Item No. 14332). It also blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner.2 Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bonhaus, D.W., Flippin, L.A., Greenhouse, R.J., et al. RS-127445: A selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br. J. Pharmacol. 127(5), 1075-1082 (1999).

    2. Bassil, A.K., Taylor, C.M., Bolton, V.J., et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br. J. Pharmacol. 158(1), 252-258 (2009).

    3. Devroye, C., Cathala, A., Di Marco, B., et al. Central serotonin2B receptor blockade inhibits cocaine-induced hyperlocomotion independently of changes of subcortical dopamine outflow. Neuropharmacology 97, 329-337 (2015).