K-14585 | CAS#880546-17-8 | PAR-2 antagonist

MedKoo Cat#: 558223 | Name: K-14585

Description:

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

K-14585 is a proteinase-activated receptor 2 antagonist. Pretreatment with K-14585 inhibited PAR(2)-mediated p65 NFkappaB phosphorylation and NFkappaB-DNA binding. K-14585 inhibited SLIGKV-stimulated IL-8 production, but given alone increased IL-8. K-14585 antagonized PAR(2) competitively, resulting in inhibition of PAR(2)-mediated signalling and physiological responses both in vitro and in vivo. K-14585 could be useful in evaluating PAR(2)-mediated biological events and might lead to a new generation of therapeutically useful antagonists.

Chemical Structure

K-14585

CAS#880546-17-8

Theoretical Analysis

MedKoo Cat#: 558223

Name: K-14585

CAS#: 880546-17-8

Chemical Formula: C51H56Cl2N8O4

Exact Mass: 914.3802

Molecular Weight: 915.96

Elemental Analysis: C, 66.88; H, 6.16; Cl, 7.74; N, 12.23; O, 6.99

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

K-14585; K 14585; K14585.

IUPAC/Chemical Name

(S)-6-amino-N-((S)-1-(benzhydrylamino)-1-oxo-3-phenylpropan-2-yl)-2-(2-(3-(1-(2,6-dichlorobenzyl)-3-(pyrrolidin-1-ylmethyl)-1H-indol-5-yl)ureido)acetamido)hexanamide

InChi Key

ADEQJSQZZXWZPW-GSVOJQHPSA-N

InChi Code

InChI=1S/C51H56Cl2N8O4/c52-42-21-14-22-43(53)41(42)34-61-33-38(32-60-27-12-13-28-60)40-30-39(24-25-46(40)61)56-51(65)55-31-47(62)57-44(23-10-11-26-54)49(63)58-45(29-35-15-4-1-5-16-35)50(64)59-48(36-17-6-2-7-18-36)37-19-8-3-9-20-37/h1-9,14-22,24-25,30,33,44-45,48H,10-13,23,26-29,31-32,34,54H2,(H,57,62)(H,58,63)(H,59,64)(H2,55,56,65)/t44-,45-/m0/s1

SMILES Code

ClC1=CC=CC(Cl)=C1CN2C(C=C3)=C(C(CN4CCCC4)=C2)C=C3NC(NCC(N[C@H](C(N[C@@H](CC5=CC=CC=C5)C(NC(C6=CC=CC=C6)C7=CC=CC=C7)=O)=O)CCCCN)=O)=O

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

Shelf Life

>2 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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 915.96 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.

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

1: Goh FG, Ng PY, Nilsson M, Kanke T, Plevin R. Dual effect of the novel peptide antagonist K-14585 on proteinase-activated receptor-2-mediated signalling. Br J Pharmacol. 2009 Dec;158(7):1695-704. doi: 10.1111/j.1476-5381.2009.00415.x. Epub . PubMed PMID: 19917067; PubMed Central PMCID: PMC2801210. 2: Kanke T, Kabeya M, Kubo S, Kondo S, Yasuoka K, Tagashira J, Ishiwata H, Saka M, Furuyama T, Nishiyama T, Doi T, Hattori Y, Kawabata A, Cunningham MR, Plevin R. Novel antagonists for proteinase-activated receptor 2: inhibition of cellular and vascular responses in vitro and in vivo. Br J Pharmacol. 2009 Sep;158(1):361-71. doi: 10.1111/j.1476-5381.2009.00342.x. PubMed PMID: 19719785; PubMed Central PMCID: PMC2795266.