PF-06447475

한글명:PF-06447475

카스 번호1527473-33-1

상품명:PF-06447475

CBNumberCB52735532

분자식C17H15N5O

포뮬러 무게305.33

MOL 파일1527473-33-1.mol

화학적 성질

녹는점	>223°C (dec.)
밀도	1.40±0.1 g/cm3(Predicted)
저장 조건	room temp
용해도	DMSO: 용해성10mg/mL, 투명
산도 계수 (pKa)	12.96±0.50(Predicted)
물리적 상태	가루
색상	흰색에서 베이지색

위험 및 안전 성명

위험품 표기	T
위험 카페고리 넘버	25
안전지침서	45
유엔번호(UN No.)	UN 2811 6.1 / PGIII

그림문자(GHS)

PF-06447475 화학적 특성, 용도, 생산

용도
PF 06447475 is a highly potent LRRK2 kinase inhibitor. Highly selective, and mobile, it is used in the treatment of Parkinson’s disease which has been linked to Leucine rich repeat kinase 2 (LRRK2) enzymes.
효소 저해제
This potent, brain penetrant and selective LRRK2 inhibitor (FW = 305.44 g/mol; CAS 1527473-33-1), also named 3-[4-(4-morpholinyl)-7Hpyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile, targets Leucine-Rich Repeat Kinase 2, IC50 = 3 nM, (encoded by the PARK8 gene), which phosphorylates Akt1 (Ser-473), suggesting that Akt1 is a convincing candidate for the physiological substrate of LRRK2. Diseaseassociated mutations forms of LRRK2 (including Arg-1441-Cys, Gly-2019- Ser, and Ile-2020-Thr) exhibit reduced interaction with, and phosphorylation of, Akt1, a finding that suggests a possible mechanism for the neurodegeneration caused by LRRK2 mutations. Therapeutic approaches to slow or block the progression of Parkinson disease (PD) do not exist. Given that genetic and biochemical studies implicate α-synuclein and leucine-rich repeat kinase 2 (LRRK2) in late-onset PD. In wild-type rats as well as transgenic [Gly-2019-Ser]-LRRK2 rats that were injected intracranially with adeno-associated viral vectors expressing human α- synuclein in the substantia nigra, those expressing [Gly-2019-Ser]-LRRK2 show exacerbated dopaminergic neurodegeneration and inflammation in response to the overexpression of α-synuclein. Both neurodegeneration and neuroinflammation associated with [Gly-2019-Ser]-LRRK2 expression were mitigated by PF-06447475, which provided neuroprotection in wildtype rats. There are no adverse pathological indications in the lung, kidney, or liver of rats treated with PF-06447475. Pharmacological inhibition of LRRK2 is well tolerated for a 4-week period of time in rats and can counteract dopaminergic neurodegeneration caused by acute α-synuclein overexpression

PF-06447475 준비 용품 및 원자재

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