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)-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-;HEK293,JHII127,3T3 cells,Inhibitor,LRRK2-G2019S,Ser935,Leucine-rich repeat kinase 2,LRRK2,parkinson’s disease,inhibit,JH II 127,LRRK2-A2016T
- CBNumber:
- CB43049255
- Molecular Formula:
- C19H21ClN6O3
- Molecular Weight:
- 416.86
- MDL Number:
- MFCD28975160
- MOL File:
- 1700693-08-8.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319 |
| Precautionary statements | P261-P305+P351+P338 |
JH-II-127 price More Price(14)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2569 | JH-II-127 ≥98% (HPLC) | 1700693-08-8 | 5MG | $123 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML2569 | JH-II-127 ≥98% (HPLC) | 1700693-08-8 | 25MG | $396 | 2024-03-01 | Buy |
| Cayman Chemical | 22905 | JH-II-127 | 1700693-08-8 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 22905 | JH-II-127 | 1700693-08-8 | 5mg | $139 | 2024-03-01 | Buy |
| Cayman Chemical | 22905 | JH-II-127 | 1700693-08-8 | 10mg | $243 | 2024-03-01 | 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 (h?ng/mL) | AUGINF (h?ng/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
JH-II-127 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29807 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32275 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38664 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39002 | 58 |
