(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide
- Product Name
- (1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide
- CAS No.
- 1246303-14-9
- Chemical Name
- (1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide
- Synonyms
- ML270;VU0359595;(1R,2R)-N-[(2S)-1-[4-(5-bromo-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]propan-2-yl]-2-phenylcyclopropane-1-carboxamide;(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide;Cyclopropanecarboxamide, N-[(1S)-2-[4-(5-bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-2-phenyl-, (1R,2R)-;(1R,2R)-N-([S]-1-{4-[5-BROMO-2-OXO-2,3-DIHYDRO-1H-BENZO(D)IMIDAZOL-1-YL]PIPERIDIN-1-YL}PROPAN-2-YL)-2-PHENYLCYCLOPROPANECARBOXAMIDE;VU0359595
- CBNumber
- CB52719857
- Molecular Formula
- C25H29BrN4O2
- Formula Weight
- 497.43
- MOL File
- 1246303-14-9.mol
(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide Property
- Density
- 1.395±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble5mg/mL, clear
- pka
- 11.11±0.30(Predicted)
- form
- powder
- color
- white to beige
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- 10955
- Product name
- VU0359595
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $40
- Updated
- 2024/03/01
- Product number
- 10955
- Product name
- VU0359595
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 10955
- Product name
- VU0359595
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $236
- Updated
- 2024/03/01
- Product number
- 10955
- Product name
- VU0359595
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $541
- Updated
- 2024/03/01
- Product number
- V787565
- Product name
- VU0359595
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide Chemical Properties,Usage,Production
Uses
VU0359595 is an inhibitor of phospholipase D1 (PLD1) which is more than 1700 fold selective over phospholipase D2 (PLD2). This complex only binds and inhibit phospholipase D though an allosteric site, but it noes not interact with the catalytic site of phospholipase D.
Biological Activity
vu0359595 is a potent and selective inhibitor of pld1.phospholipase d (pld) isozymes mediate phospholipid hydrolysis and transphosphatidylation. until now, two mammalian isoforms of pld, pld1, and pld2, have been identified. it has been identified that pld has been implicated in a human cancer cell progression, actin cytoskeleton reorganization and cell motility [1].
in vitro
vu0359595 was an inhibitor of pld1 with an ic50 of 3.7 nm. vu0359595 showed >1,700-fold selectivity over pld2. the ic50 of was vu0359595 against pld2 was 6.4 μm [1]. preliminary evidence has demonstrated that vu0359595 showed no interaction with the catalytic site of pld, but may bind and inhibit pld through an allosteric site [1]. at 500 nm, vu0359595 significantly reduced the pld activity in astroglial cultures from wild-type mice by 58% [2]. in cells stimulated by 1% fcs, vu0359595 decreased cell proliferation in wild-type and pld2-deficient cells at a concentration of 500 nm [2]. vu0359595 (500 nm) significantly reduced cell growth in cells stimulated by either mitogen [2].
References
[1] lewis j a, scott s a, lavieri r, et al. design and synthesis of isoform-selective phospholipase d (pld) inhibitors. part i: impact of alternative halogenated privileged structures for pld1 specificity[j]. bioorganic & medicinal chemistry letters, 2009, 19(7): 1916-1920.
[2] burkhardt u, beyer s, klein j. role of phospholipases d1 and 2 in astroglial proliferation: effects of specific inhibitors and genetic deletion[j]. european journal of pharmacology, 2015, 761: 398-404.
(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide Preparation Products And Raw materials
Raw materials
Preparation Products
(1R,2R)-N-([S]-1-{4-[5-broMo-2-oxo-2,3-dihydro-1H-benzo(d)iMidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxaMide Suppliers
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