MK-0752

Modify Date: 2024-01-02 19:46:41

MK-0752 structure	Common Name	MK-0752
	CAS Number	471905-41-6	Molecular Weight	442.904
	Density	1.4±0.1 g/cm3	Boiling Point	616.9±55.0 °C at 760 mmHg
	Molecular Formula	C₂₁H₂₁ClF₂O₄S	Melting Point	N/A
	MSDS	N/A	Flash Point	326.9±31.5 °C

Use of MK-0752

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.IC50 value: 5 nM (reduces Aβ40 production) [1]Target: γ-secretasein vitro: MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells [1]. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation [2]. in vivo: MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17 [1]. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain [2].

Name	cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
Synonym	More Synonyms

Description	MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.IC50 value: 5 nM (reduces Aβ40 production) [1]Target: γ-secretasein vitro: MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells [1]. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation [2]. in vivo: MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17 [1]. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain [2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> γ-secretase Signaling Pathways >> Stem Cell/Wnt >> γ-secretase Research Areas >> Neurological Disease
References	[1]. Cook JJ, et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci, 2010, 30(19), 6743-6750. [2]. Harrison H, et al. Regulation of breast cancer stem cell activity by signaling through the Notch4 receptor. Cancer Res, 2010, 70(2), 709-718.

Description

Related Catalog

Signaling Pathways >> Neuronal Signaling >> γ-secretase

Signaling Pathways >> Stem Cell/Wnt >> γ-secretase

Research Areas >> Neurological Disease

References

[1]. Cook JJ, et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci, 2010, 30(19), 6743-6750.

[2]. Harrison H, et al. Regulation of breast cancer stem cell activity by signaling through the Notch4 receptor. Cancer Res, 2010, 70(2), 709-718.

Density	1.4±0.1 g/cm3
Boiling Point	616.9±55.0 °C at 760 mmHg
Molecular Formula	C₂₁H₂₁ClF₂O₄S
Molecular Weight	442.904
Flash Point	326.9±31.5 °C
Exact Mass	442.081726
PSA	79.82000
LogP	4.41
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.569
Storage condition	-20℃

Precursor 9
CAS#:656810-86-5 cis-1-[4-[(4-ch... CAS#:7758-19-2 Sodium chlorite CAS#:5329-14-6 Sulfamic acid CAS#:106-54-7 4-Chlorothiophenol
CAS#:470716-52-0 2-{[(4-Chloroph... CAS#:470716-51-9 4-chlorophenyl ... CAS#:85117-99-3 2,5-Difluoroben... CAS#:471903-20-5 4-(4-chlorophen...
CAS#:471905-61-0 2-{1-[(4-Chloro...
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