JH-II-127
- CAS No.
- 1700693-08-8
- Chemical Name:
- JH-II-127
- Synonyms
- JH-II-127;JH-II-127, 10 mM in DMSO;2-anilino-4-methylamino-5-chloropyrrolopyrimidine;2-ANILINO-4-METHYLAMINO-5-CHLOROPYRROLOPYRIMIDINE;JH-II127;JH-II 127;(4-((5-Chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholi;(4-((5-chloro-4-(methylamino)-3h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone;(4-((5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone;[4-[[5-Chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinyl-methanone;[4-[[5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone;Methanone, [4-[[5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinyl-
- CBNumber:
- CB43049255
- Molecular Formula:
- C19H21ClN6O3
- Molecular Weight:
- 416.86
- MDL Number:
- MFCD28975160
- MOL File:
- 1700693-08-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Melting point | >166°C (dec.) |
|---|---|
| Density | 1.458±0.06 g/cm3(Predicted) |
| storage temp. | Refrigerator |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| pka | 12.49±0.50(Predicted) |
| form | Solid |
| color | White to Pale Beige |
| InChI | 1S/C19H21ClN6O3/c1-21-16-15-12(20)10-22-17(15)25-19(24-16)23-13-4-3-11(9-14(13)28-2)18(27)26-5-7-29-8-6-26/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24,25) |
| InChIKey | HUEKBQXFNHWTQQ-UHFFFAOYSA-N |
| SMILES | Clc1c2c(nc([nH]c2NC)Nc3c(cc(cc3)C(=O)N4CCOCC4)OC)nc1 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) | ![]() GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
JH-II-127 price More Price(37)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2569 | JH-II-127 ≥98% (HPLC) | 1700693-08-8 | 5MG | $115 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML2569 | JH-II-127 ≥98% (HPLC) | 1700693-08-8 | 25MG | $371 | 2026-04-30 | Buy |
| Cayman Chemical | 22905 | JH-II-127 ≥98% | 1700693-08-8 | 1mg | $36 | 2026-04-30 | Buy |
| Cayman Chemical | 22905 | JH-II-127 ≥98% | 1700693-08-8 | 5mg | $153 | 2026-04-30 | Buy |
| Cayman Chemical | 22905 | JH-II-127 ≥98% | 1700693-08-8 | 10mg | $268 | 2026-04-30 | Buy |
JH-II-127 Chemical Properties, Uses, Production
Description
JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2). It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 μM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.
Uses
JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor.
in vivo
JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain[1].
| matrix | route | Tmax (h) | C0/Cmax (ng/mL) | AUCLast (hng/mL) | AUGINF (hng/mL) | T1/2 (h) | CL (mL/min/kg) | Vss (L/kg) |
| plasma | IV (2 mg/kg) | - | 1604.47 | 532.67 | 535.57 | 0.66 | 62.24 | 1.73 |
| plasma | PO (10 mg/kg) | 1 | 802.72 | 3094.58 | 3867.07 | - | - | - |
| brain | IV (2 mg/kg) | - | 1343.6 | 239.31 | 246.47 | 0.23 | 135.24 | 1.7 |
| brain | PO (10 mg/kg) | 1 | 247.35 | 688.21 | 762.38 | - | - | - |
| Animal Model: | Wild type male C57BL/6 mice[1]. |
| Dosage: | 2 mg/kg (for i.v.); 10 mg/kg (for p.o.); 10, 30, 100 mg/kg (for i.p.) |
| Administration: | Intravenous and intraperitoneal injection; oral administration; single. |
| Result: | Led to near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain when at 100 mg/kg of i.p. and near complete inhibition in all tissues at 30 mg/kg but only partial inhibition in brain at the 10 mg/kg dose. Demonstrated good oral bioavailability. |
storage
Store at -20°C
References
[1] JOHN M. HATCHER. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor[J]. ACS Medicinal Chemistry Letters, 2015, 6 5: 584-589. DOI: 10.1021/acsmedchemlett.5b00064
JH-II-127 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| UHN Shanghai Research & Development Co., Ltd. | 021-58958002 18930822973 | sales@uhnshanghai.com | China | 997 | 58 |
| AdooQ Bioscience CHINA | 025-58849295 | info@adooq.cn | China | 2981 | 60 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4860 | 55 | |
| Shanghaizehan biopharma technology co., Ltd. | 021-61350663 13052117465 | sales@zehanbiopharma.com | China | 989 | 55 |
| ShangHai Siyan Biological Technology Co., Ltd. | 021-50908862,442785678,326799392 18721037013 | siyansales@126.com | China | 9612 | 58 |
| Guangzhou QiYun Biotechnology Co., Ltd. | 020-61288194 61288195 | 505721671@qq.com | China | 3853 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
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