PAC 14028

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

MedKoo CAT#: 529207

CAS#: 1005168-10-4

Description: PAC 14028, also known as Asivatrep, is a vanilloid VR1 receptor (TRPV1) antagonist potentially for the treatment of pruritus and acne


Price and Availability

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PAC 14028 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 529207
Name: PAC 14028
CAS#: 1005168-10-4
Chemical Formula: C21H22F5N3O3S
Exact Mass: 491.1302
Molecular Weight: 491.47
Elemental Analysis: C, 51.32; H, 4.51; F, 19.33; N, 8.55; O, 9.77; S, 6.52


Synonym: PAC 14028; PAC-14028; PAC14028; Asivatrep

IUPAC/Chemical Name: (R,E)-N-(1-(3,5-difluoro-4-(methylsulfonamido)phenyl)ethyl)-3-(2-propyl-6-(trifluoromethyl)pyridin-3-yl)acrylamide

InChi Key: UKGJZDSUJSPAJL-YPUOHESYSA-N

InChi Code: InChI=1S/C21H22F5N3O3S/c1-4-5-17-13(6-8-18(28-17)21(24,25)26)7-9-19(30)27-12(2)14-10-15(22)20(16(23)11-14)29-33(3,31)32/h6-12,29H,4-5H2,1-3H3,(H,27,30)/b9-7+/t12-/m1/s1

SMILES Code: O=C(N[C@@H](C1=CC(F)=C(NS(=O)(C)=O)C(F)=C1)C)/C=C/C2=CC=C(C(F)(F)F)N=C2CCC


Technical Data

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).

Harmonized System Code:
293490


References

1: Park YH, Joo KM, Woo BY, Son ED, Byun SY, Shin HJ, Lee KW, Park YH, Lim KM. Oral and topical pharmacokinetic studies of a novel TRPV1 antagonist, PAC-14028 in rats and minipigs using liquid chromatography/tandem mass spectrometric method. J Pharm Biomed Anal. 2012 Mar 5;61:8-14. doi: 10.1016/j.jpba.2011.11.011. PubMed PMID: 22169466.

2: Lim KM, Park YH. Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6. doi: 10.1007/s12272-012-0321-6. PubMed PMID: 22477184.

3: Yun JW, Seo JA, Jeong YS, Bae IH, Jang WH, Lee J, Kim SY, Shin SS, Woo BY, Lee KW, Lim KM, Park YH. TRPV1 antagonist can suppress the atopic dermatitis-like symptoms by accelerating skin barrier recovery. J Dermatol Sci. 2011 Apr;62(1):8-15. doi: 10.1016/j.jdermsci.2010.10.014. PubMed PMID: 21345654.

4: Yun JW, Seo JA, Jang WH, Koh HJ, Bae IH, Park YH, Lim KM. Antipruritic effects of TRPV1 antagonist in murine atopic dermatitis and itching models. J Invest Dermatol. 2011 Jul;131(7):1576-9. doi: 10.1038/jid.2011.87. PubMed PMID: 21471988.