PAC-14028

Product Name: PAC-14028
CAS No.: 1005168-10-4
Chemical Name: PAC-14028
Synonyms: PAC-14028;PAC14028; PAC 14028;Xanthine Impurity 8;Asivatrep (PAC-14028);2-Propenamide, N-[(1R)-1-[3,5-difluoro-4-[(methylsulfonyl)amino]phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)-3-pyridinyl]-, (2E)-
CBNumber: CB53122034
Molecular Formula: C21H22F5N3O3S
Formula Weight: 491.47
MOL File: 1005168-10-4.mol

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PAC-14028 Property

Density: 1.381±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 50 mg/mL (101.74 mM)
form: Solid
pka: 7.41±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene

Product number: CS-6239
Product name: Asivatrep
Purity: 95.14%
Packaging: 1mg
Price: $180
Updated: 2021/12/16

ChemScene

Product number: CS-6239
Product name: Asivatrep
Purity: 95.14%
Packaging: 5mg
Price: $420
Updated: 2021/12/16

ChemScene

Product number: CS-6239
Product name: Asivatrep
Purity: 95.14%
Packaging: 50mg
Price: $1800
Updated: 2021/12/16

DC Chemicals

Product number: DC10399
Product name: PAC-14028
Purity: >98%
Packaging: 100mg
Price: $900
Updated: 2021/12/16

DC Chemicals

Product number: DC10399
Product name: PAC-14028
Purity: >98%
Packaging: 250mg
Price: $1800
Updated: 2021/12/16

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PAC-14028 Chemical Properties,Usage,Production

Uses

Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

in vivo

Asivatrep (PAC-14028) shows a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively suggesting that Asivatrep (PAC-14028) is relatively well-absorbed through oral route^[1]. Asivatrep (PAC-14028) could inhibit capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations. This potent TRPV1 antagonistic activity in keratinocytes is manifested in vivo as the blockade of capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice^[3].

References

[1] Park YH, et al. 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
[2] Lim KM, et al. 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
[3] Yun JW, et al. 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

PAC-14028 Preparation Products And Raw materials

Raw materials

Preparation Products

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PAC-14028 Suppliers

China 29 United States 2 Global 31

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PAC-14028

PAC14028; PAC 14028

2-Propenamide, N-[(1R)-1-[3,5-difluoro-4-[(methylsulfonyl)amino]phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)-3-pyridinyl]-, (2E)-

Asivatrep (PAC-14028)

Xanthine Impurity 8

1005168-10-4

C21H22F5N3O3S