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SML2411

Sigma-Aldrich

KPR-2579

≥98% (HPLC)

Sinonimo/i:

(αR)-α-[Benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-benzeneacetamide, N-((R)-2-Amino-2-oxo-1-phenylethyl)-N-((R)-1-(3,5-difluorophenyl)ethyl)benzamide, N-((R)-Carbamoylphenylmethyl)-N-[(R)-1-(3,5-difluorophenyl)ethyl]benzamide

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About This Item

Formula empirica (notazione di Hill):
C23H20F2N2O2
Numero CAS:
1801742-41-5
Peso molecolare:
394.41
Codice UNSPSC:
12352200

Saggio

≥98% (HPLC)

Stato

powder

Attività ottica

[α]/D +124 to +136°, c = c=1 in chloroform-d

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(C1=CC=CC=C1)N([C@H](C)C2=CC(F)=CC(F)=C2)[C@H](C3=CC=CC=C3)C(N)=O

InChI

1S/C23H20F2N2O2/c1-15(18-12-19(24)14-20(25)13-18)27(23(29)17-10-6-3-7-11-17)21(22(26)28)16-8-4-2-5-9-16/h2-15,21H,1H3,(H2,26,28)/t15-,21-/m1/s1
NNXPFEMWLZLAHM-QVKFZJNVSA-N

Azioni biochim/fisiol

KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs), stimulated by acetic acid (AA).
KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca2+ response in human/rat CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca2+ influx using hTRPA1, hTRPV1, or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects.
Potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist with good selectivity, in vivo efficacy and oral bioavailability.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Jun-Ichi Kobayashi et al.
Bioorganic & medicinal chemistry, 25(2), 727-742 (2016-12-15)
Transient receptor potential melastatin 8 (TRPM8) is activated by innocuous cold and chemical substances, and antagonists of this channel have been considered to be effective for pain and urinary diseases. N-(3-aminopropyl)-2-{[(3-methylphenyl)methyl]oxy}-N-(2-thienylmethyl)benzamide hydrochloride (AMTB), a TRPM8 antagonist, was proposed to be
KPR-2579, a novel TRPM8 antagonist, inhibits acetic acid-induced bladder afferent hyperactivity in rats
Aizawa N, et al.
Neurourology and Urodynamics, 37(5), 1633-1640 (2018)
Naoki Aizawa et al.
Neurourology and urodynamics, 37(5), 1633-1640 (2018-02-22)
Transient receptor potential melastatin 8 (TRPM8) is proposed to be a promising therapeutic target for hypersensitive bladder disorders. We examined the effects of KPR-2579, a novel selective TRPM8 antagonist, on body temperature and on mechanosensitive bladder single-unit afferent activities (SAAs)

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