SDZ NKT 343
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MedKoo CAT#: 574400

CAS#: 180046-99-5

Description: SDZ NKT 343 is a highly selective human tachykinin NK1 receptor antagonist that antagonizes SP-induced Ca2+ efflux in vitro and inhibits mechanical hyperalgesia in vivo.

Chemical Structure

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SDZ NKT 343
CAS# 180046-99-5
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574400
Name: SDZ NKT 343
CAS#: 180046-99-5
Chemical Formula: C33H33N5O5
Exact Mass: 579.25
Molecular Weight: 579.660
Elemental Analysis: C, 68.38; H, 5.74; N, 12.08; O, 13.80

Price and Availability

Size Price Availability Quantity
10mg USD 430 2 Weeks
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Synonym: SDZ NKT 343

IUPAC/Chemical Name: 1-[[(2-Nitrophenyl)amino]carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide

InChi Key: UYLNUSYIZWUOLL-KYJUHHDHSA-N

InChi Code: InChI=1S/C33H33N5O5/c1-36(22-23-10-3-2-4-11-23)30(21-24-17-18-25-12-5-6-13-26(25)20-24)32(40)35-31(39)29-16-9-19-37(29)33(41)34-27-14-7-8-15-28(27)38(42)43/h2-8,10-15,17-18,20,29-30H,9,16,19,21-22H2,1H3,(H,34,41)(H,35,39,40)/t29-,30-/m0/s1

SMILES Code: O=C(NC([C@H]1N(C(NC2=CC=CC=C2[N+]([O-])=O)=O)CCC1)=O)[C@H](CC3=CC=C4C=CC=CC4=C3)N(C)CC5=CC=CC=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO and ethanol

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: SDZ NKT 343 is a highly selective human tachykinin NK1 receptor antagonist (IC50 values are 0.62 and 451 nM for human and rat receptors, respectively) that displays >130-fold selectivity over human NK2 and NK3 receptors.
In vitro activity: To be determined
In vivo activity: The findings of this study suggest that the blockade of neurokinin 1 receptors by SDZ NKT 343 selectively reduces sensitized responses to innocuous mechanical stimuli without impacting responses to noxious mechanical stimuli.In a model of capsaicin-induced sensitization of spinothalamic tract cells in monkeys, there was a significant reversal of the increased response to brushing, while the heightened background activity and response to pressure remained unaffected after SDZ NKT 343 treatment. Reference: Exp Brain Res. 1998 Aug;121(3):355-8. https://pubmed.ncbi.nlm.nih.gov/9746141/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 58.0 100.00
Ethanol 58.0 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 579.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Campbell EA, Gentry C, Patel S, Kidd B, Cruwys S, Fox AJ, Urban L. Oral anti-hyperalgesic and anti-inflammatory activity of NK(1) receptor antagonists in models of inflammatory hyperalgesia of the guinea-pig. Pain. 2000 Sep;87(3):253-263. doi: 10.1016/S0304-3959(00)00288-8. PMID: 10963905. 2. Rees H, Sluka KA, Urban L, Walpole CJ, Willis WD. The effects of SDZ NKT 343, a potent NK1 receptor antagonist, on cutaneous responses of primate spinothalamic tract neurones sensitized by intradermal capsaicin injection. Exp Brain Res. 1998 Aug;121(3):355-8. doi: 10.1007/s002210050468. PMID: 9746141.
In vitro protocol: To be determined
In vivo protocol: 1. Campbell EA, Gentry C, Patel S, Kidd B, Cruwys S, Fox AJ, Urban L. Oral anti-hyperalgesic and anti-inflammatory activity of NK(1) receptor antagonists in models of inflammatory hyperalgesia of the guinea-pig. Pain. 2000 Sep;87(3):253-263. doi: 10.1016/S0304-3959(00)00288-8. PMID: 10963905. 2. Rees H, Sluka KA, Urban L, Walpole CJ, Willis WD. The effects of SDZ NKT 343, a potent NK1 receptor antagonist, on cutaneous responses of primate spinothalamic tract neurones sensitized by intradermal capsaicin injection. Exp Brain Res. 1998 Aug;121(3):355-8. doi: 10.1007/s002210050468. PMID: 9746141.

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1. Walpole et al (1998) Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br.J.Pharmacol. 124 83 PMID: 9630347

2. Walpole et al (1998) 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N-methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J.Med.Chem. 41 3159 PMID: 9703462

3. Campbell et al (1998) Selective neurokinin-1 receptor antagonists are anti-hyperalgesic in a model of neuropathic pain in the guinea-pig. Neuroscience. 87 527 PMID: 9758219