Free shipping on all orders over $ 500

SB 223412

Cat. No. M7258
SB 223412 Structure
Synonym:

Talnetant

Size Price Availability Quantity
10mg USD 135  USD150 In stock
50mg USD 535.5  USD595 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SB 223412 is a potent and selective non-peptide NK3 receptor antagonist (Ki values are 1, 144 and >100000 nM for human NK3, NK2 and NK1 receptors respectively). Selective over a panel of >60 receptors, enzymes and ion channels at concentrations of 1 or 10 μM. Inhibits NKB-induced Ca2+ mobilization in vitro (IC50 = 16.6 nM) and inhibits NK3-agonist-induced behavioral responses in vivo. Orally active and brain penetrant.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 382.45
Formula C25H22N2O2
CAS Number 174636-32-9
Purity >99%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
References

In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia.
Dawson LA, et al. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. PMID: 17728699.

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).
Giardina GA, et al. J Med Chem. 1999 Mar 25;42(6):1053-65. PMID: 10090788.

Related Neurokinin Receptor Products
[Leu31,Pro34]-NPY TFA (human,rat)

[Leu31,Pro34]-NPY TFA (human,rat) is a specific neuropeptide Y1 receptor agonist.

Vapreotide acetate

Vapreotide acetate (BMY-41606 acetate; RC160 acetate) is a neurokinin-1 (NK1) receptor antagonist with IC50 value of 330 nM.

Ibodutant

Ibodutant (MEN15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.

Serlopitant

Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.

Substance P

Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB 223412, Talnetant supplier, Neurokinin Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.