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| Cas No.: | 471905-41-6 |
| Chemical Name: | 3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid |
| Synonyms: | MK-0752,MK 0752 |
| SMILES: | C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl |
| Formula: | C21H21ClF2O4S |
| M.Wt: | 442.9 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| Publication: | Wang, C., Xue, Y., Markovic, T.et al. Blood–brain-barrier-crossing lipid nanoparticles for mRNA delivery to the central nervous system. Nat. Mater. (2025). |
| Description: | MK-0752 is a moderately potent γ-secretase inhibitor, it is used as a head group of MK16 which is a a novel blood-brain barrier (BBB)-crossing lipid nanoparticle (BLNP) platform developed for efficient mRNA delivery to the central nervous system (CNS). |
| 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]. |
| In 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]. |