2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide
- Product Name
- 2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide
- CAS No.
- 1375465-91-0
- Chemical Name
- 2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide
- Synonyms
- CS-2244;ACY-738;ACY 738; ACY738;ACY-738, 10 mM in DMSO;ACY738;ACY-738;ACY 738;2-(1-phenylcyclopropylamino)-N-hydroxypyrimidine-5-carboxamide;N-Hydroxy-2-[(1-phenylcyclopropyl)amino]-5-pyrimidinecarboxamide;N-hydroxy-2-[(1-phenylcyclopropyl)amino]pyrimidine-5-carboxamide;5-Pyrimidinecarboxamide, N-hydroxy-2-[(1-phenylcyclopropyl)amino]-;2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide
- CBNumber
- CB22742795
- Molecular Formula
- C14H14N4O2
- Formula Weight
- 270.29
- MOL File
- 1375465-91-0.mol
2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide Property
- Density
- 1.433±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:32.0(Max Conc. mg/mL);118.39(Max Conc. mM)
- form
- A crystalline solid
- pka
- 7.75±0.10(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 28282
- Product name
- ACY-738
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 28282
- Product name
- ACY-738
- Packaging
- 25mg
- Price
- $819
- Updated
- 2024/03/01
- Product number
- 28282
- Product name
- ACY-738
- Packaging
- 5mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- 28282
- Product name
- ACY-738
- Packaging
- 10mg
- Price
- $419
- Updated
- 2024/03/01
- Product number
- CS-5149
- Product name
- ACY-738
- Purity
- 98.75%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2021/12/16
2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide Chemical Properties,Usage,Production
Description
ACY-738 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 1.7 nM). It is selective for HDAC6 over HDAC1-3 (IC50s = 94, 128, and 218 nM, respectively). ACY-738 (5 mg/kg) increases acetylation of α-tubulin in mouse brain. It increases exploratory activity in a novel open-field test and reduces immobility time in a tail suspension test in wild-type, but not neural cell-selective HDAC6 knockout, mice when administered at a dose of 50 mg/kg, indicating anxiolytic and antidepressant-like activity, respectively. ACY-738 (100 mg/kg in the diet) attenuates decreases in caudal nerve sensory nerve action potential (SNAP) amplitude and increases in hind paw mechanical hypersensitivity in a mouse model of peripheral neuropathy induced by vincristine . It decreases hepatorenal cystogenesis in a rat model of polycystic liver disease when administered at a dose of 30 mg/kg.
Uses
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
in vivo
ACY-738 (5mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment[1]. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels[2].
IC 50
HDAC6: 1.7 nM (IC50); HDAC1: 94 nM (IC50); HDAC2: 128 nM (IC50); HDAC3: 218 nM (IC50)
References
[1] Jochems J, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. DOI:10.1038/npp.2013.207
[2] Regna NL, et al. Specific HDAC6 inhibition by ACY-738 reduces SLE pathogenesis in NZB/W mice. Clin Immunol. 2016 Jan;162:58-73. DOI:10.1016/j.clim.2015.11.007
[3] Mithraprabhu S, et al. Histone deacetylase (HDAC) inhibitors as single agents induce multiple myeloma cell death principally through the inhibition of class I HDAC. Br J Haematol. 2013 Aug;162(4):559-62. DOI:10.1111/bjh.12388
2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide manufacturers
- Product
- 2-(1-Phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid hydroxyamide 1375465-91-0
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-03