Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester
![Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester Structure](CAS/20200611/GIF/1445656-91-6.gif)
- CAS No.
- 1445656-91-6
- Chemical Name:
- Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester
- Synonyms
- LEO 39652;isobutyl 1-(8-methoxy-5-(1-oxo-1,3-dihydroisobenzofuran-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropane-1-carboxylate;Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester
- CBNumber:
- CB98100860
- Molecular Formula:
- C23H23N3O5
- Molecular Weight:
- 421.45
- MDL Number:
- MFCD33023450
- MOL File:
- 1445656-91-6.mol
Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0138693 | LEO39652 99.11% | 1445656-91-6 | 5mg | $450 | 2021-12-16 | Buy |
| ChemScene | CS-0138693 | LEO39652 99.11% | 1445656-91-6 | 10mg | $800 | 2021-12-16 | Buy |
| ChemScene | CS-0138693 | LEO39652 99.11% | 1445656-91-6 | 25mg | $1650 | 2021-12-16 | Buy |
| ChemScene | CS-0138693 | LEO39652 99.11% | 1445656-91-6 | 50mg | $2550 | 2021-12-16 | Buy |
| ChemScene | CS-0138693 | LEO39652 99.11% | 1445656-91-6 | 100mg | $3800 | 2021-12-16 | Buy |
Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester Chemical Properties,Uses,Production
Biological Activity
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1]. LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin[2]. LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1].Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg)[1].
References
[1]. Jens Larsen, et al. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3 H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel "Dual-Soft" PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis. J Med Chem. 2020 Dec 10;63(23):14502-14521. [2]. Stefan Eirefelt, et al. Evaluating Dermal Pharmacokinetics and Pharmacodymanic Effect of Soft Topical PDE4 Inhibitors: Open Flow Microperfusion and Skin Biopsies. Pharm Res. 2020 Nov 13;37(12):243.
Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
Cyclopropanecarboxylic acid, 1-[5-(1,3-dihydro-1-oxo-5-isobenzofuranyl)-8-methoxy[1,2,4]triazolo[1,5-a]pyridin-2-yl]-, 2-methylpropyl ester Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Yujinpharma(Tianjin) Technology Co.,Ltd. | 13370351217 kungfu1217@1 | kungfu1217@163.com | China | 9693 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| Birdo (Shanghai) Medical Technology Co., Ltd. | 021-021-021-58099077-8102-8041-8041 18601625411 | sales@birdotech.com | China | 8468 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
| Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd. | 13771642864 | snhuyu_2008@126.com | China | 1027 | 58 |
| RD International Technology Co., Limited | 18988968278 | sales@ubiochem.com | China | 9146 | 58 |