MedKoo Cat#: 574400 | Name: SDZ NKT 343
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

SDZ NKT 343
SDZ NKT 343
CAS#180046-99-5

Theoretical Analysis

MedKoo Cat#: 574400

Name: SDZ NKT 343

CAS#: 180046-99-5

Chemical Formula: C33H33N5O5

Exact Mass: 579.2482

Molecular Weight: 579.66

Elemental Analysis: C, 68.38; H, 5.74; N, 12.08; O, 13.80

Price and Availability

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10mg USD 600.00 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
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/
Solvent mg/mL mM
Solubility
DMSO 58.0 100.00
Ethanol 58.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.
1: Lipponen A, Paananen J, Puhakka N, Pitkänen A. Analysis of Post-Traumatic Brain Injury Gene Expression Signature Reveals Tubulins, Nfe2l2, Nfkb, Cd44, and S100a4 as Treatment Targets. Sci Rep. 2016 Aug 17;6:31570. doi: 10.1038/srep31570. PMID: 27530814; PMCID: PMC4987651. 2: Haneda E, Higuchi M, Maeda J, Inaji M, Okauchi T, Ando K, Obayashi S, Nagai Y, Narazaki M, Ikehira H, Nakao R, Zhang MR, Suzuki K, Suzuki H, Suhara T. In vivo mapping of substance P receptors in brains of laboratory animals by high- resolution imaging systems. Synapse. 2007 Apr;61(4):205-15. doi: 10.1002/syn.20363. PMID: 17230554. 3: 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. 4: Campbell EA, Gentry CT, Patel S, Panesar MS, Walpole CS, Urban L. Selective neurokinin-1 receptor antagonists are anti-hyperalgesic in a model of neuropathic pain in the guinea-pig. Neuroscience. 1998 Dec;87(3):527-32. doi: 10.1016/s0306-4522(98)00318-2. PMID: 9758219. 5: 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. 6: Walpole C, Ko SY, Brown M, Beattie D, Campbell E, Dickenson F, Ewan S, Hughes GA, Lemaire M, Lerpiniere J, Patel S, Urban L. 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. 1998 Aug 13;41(17):3159-73. doi: 10.1021/jm970499g. PMID: 9703462. 7: Walpole CS, Brown MC, James IF, Campbell EA, McIntyre P, Docherty R, Ko S, Hedley L, Ewan S, Buchheit KH, Urban LA. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br J Pharmacol. 1998 May;124(1):83-92. doi: 10.1038/sj.bjp.0701806. PMID: 9630347; PMCID: PMC1565365.