Emixustat hydrochloride
- Product Name
- Emixustat hydrochloride
- CAS No.
- 1141934-97-5
- Chemical Name
- Emixustat hydrochloride
- Synonyms
- ACU-4429;Emixustat;Emixustat (ACU-4429);Cefradine Impurity 20;ACU-4429 hydrochloride;Emixustat Hydrochlorde;Emixustat hydrochloride;ACU4429;ACU 4429;ACU-4429;Emixustat hydrochloride, 10 mM in DMSO;(R)-3-Amino-1-(3-(cyclohexylmethoxy)phenyl)propan-1-ol hydrochloride
- CBNumber
- CB82682235
- Molecular Formula
- C16H26ClNO2
- Formula Weight
- 299.83614
- MOL File
- 1141934-97-5.mol
Emixustat hydrochloride Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:44.0(Max Conc. mg/mL);146.75(Max Conc. mM)
- form
- A crystalline solid
- color
- White to off-white
- InChI
- InChI=1/C16H25NO2.ClH/c17-10-9-16(18)14-7-4-8-15(11-14)19-12-13-5-2-1-3-6-13;/h4,7-8,11,13,16,18H,1-3,5-6,9-10,12,17H2;1H/t16-;/s3
- InChIKey
- BPZWRYOUJMDQSY-LSQUZMQTNA-N
- SMILES
- [C@@H](C1=CC=CC(OCC2CCCCC2)=C1)(O)CCN.[H]Cl |&1:0,r|
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.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CD31004484
- Product name
- Emixustathydrochloride
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CD31004484
- Product name
- Emixustathydrochloride
- Purity
- 98+%
- Packaging
- 10mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CM294557
- Product name
- Emixustathydrochloride
- Purity
- 98%
- Packaging
- 100mg
- Price
- $1145
- Updated
- 2021/12/16
- Product number
- DC9771
- Product name
- Emixustat(ACU-4429)
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1700
- Updated
- 2021/12/16
- Product number
- DC9771
- Product name
- Emixustat(ACU-4429)
- Purity
- >98%
- Packaging
- 1g
- Price
- $3500
- Updated
- 2021/12/16
Emixustat hydrochloride Chemical Properties,Usage,Production
Uses
Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD)[1][2][3][4].
in vivo
Emixustat (1-10 mg/kg, oral administration, single dose, or twice daily for 6 days; 1 mg/kg, i.p., measurement after 30-60 minutes) reduced cation influx and oxygen consumption in the retinas of brown Norway rats under dark adaptation conditions[3]. Emixustat (0.03-3.0 mg/kg, intravenous injection, once daily for 5 days) inhibits neovascularization and protects the retina in the oxygen-induced retinopathy mouse model[4].
| Animal Model: | Brown norway rats (200-300 g, 3 months old)[3] |
| Dosage: | 1, 5 or 10 mg/kg |
| Administration: | Oral gavage (p.o.), single dose (1, 10 mg/kg), 2 hours followed by 4 hours of dark adaptation, or twice a day for 6 days (5 mg/kg) |
| Result: | Reduced the conductance of the retinal cation channels after dark adaptation. |
| Animal Model: | Brown norway rats (200-300 g, 3 months old)[3] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection (i.v.), retinal PO2 was measured 30-60 min later |
| Result: | Reduced the oxygen consumption during dark adaptation. |
| Animal Model: | Oxygen-induced retinopathy (OIR) mice model (BALB/c and 129/Sv / C57BL/6 mixed background) |
| Dosage: | 0.03, 0.1, 0.3, 1.0, 3.0 mg/kg |
| Administration: | Intravenous injection (i.v.), once daily for 5 days |
| Result: | Dose-dependently reduced retinal neovascularization. |
References
[1] Kiser PD, et al. Catalytic mechanism of a retinoid isomerase essential for vertebrate vision. Nat Chem Biol. 2015 Jun;11(6):409-15. DOI:10.1038/nchembio.1799
[2] Kubota R, et al. Phase 1, dose-ranging study of emixustat hydrochloride (ACU-4429), a novel visual cycle modulator, in healthy volunteers. Retina. 2014 Mar;34(3):603-9. DOI:10.1097/01.iae.0000434565.80060.f8
[3] Kubota R, et al. Emixustat Reduces Metabolic Demand of Dark Activity in the Retina. Invest Ophthalmol Vis Sci. 2019 Nov 1;60(14):4924-4930. DOI:10.1167/iovs.19-28194
[4] Bavik C, et al. Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity. PLoS One. 2015 May 13;10(5):e0124940. DOI:10.1371/journal.pone.0124940
Emixustat hydrochloride Preparation Products And Raw materials
Raw materials
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