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Alfaxalone

Alfaxalone Structure
CAS No.
23930-19-0
Chemical Name:
Alfaxalone
Synonyms
gr2/234;ALFAXALONE;ALPHAXALONE;Alphaxolone;ALFAXALONE USP/EP/BP;5A-pregnan-3A-ol-11,20-dione;5α-Pregnan-3α-ol-11,20-dione;3-hydroxypregnane-11,20-dione;5α-PREGNAN-3α-OL-11, 20-DIONE;3α-Hydroxy-5α-pregnane-11,12-dione
CBNumber:
CB0756297
Molecular Formula:
C21H32O3
Molecular Weight:
332.48
MOL File:
23930-19-0.mol
Modify Date:
2024/4/1 18:08:31

Alfaxalone Properties

Melting point 172-174°
alpha D26 +113.4° (c = 1.2 in chloroform).
Boiling point 409.59°C (rough estimate)
Density 1.0834 (rough estimate)
refractive index 1.5192 (estimate)
storage temp. Store at RT
solubility chloroform: ≥5 mg/mL, clear, colorless
form powder
pka 15.05±0.70(Predicted)
color white
InChI InChI=1/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/s3
InChIKey DUHUCHOQIDJXAT-YYJIQYHHNA-N
SMILES [C@]12([H])C(=O)C[C@]3(C)[C@H](CC[C@@]3([H])[C@]1([H])CC[C@@]1([H])C[C@H](O)CC[C@]21C)C(=O)C |&1:0,5,7,10,12,16,19,23,r|

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310
Hazard Codes  Xn
Risk Statements  22
Safety Statements  22-36
RIDADR  UN 2811 6.1/PG 3
WGK Germany  3
RTECS  TU4157800
Toxicity LD50 i.v. in mice: 43 mg/kg (Al-Khawashki)

Alfaxalone Chemical Properties,Uses,Production

Description

Alfaxalone (Alfaxan, Vetoquinol) is a neurologically active steroid compound that induces general anaesthesia. Alfaxalone exerts its action by binding to GABA receptors on the neuronal cell surface, affecting cell membrane chloride ion transport. It has negligible analgesic properties at therapeutic doses. Alfaxalone may be administered either intravenously or intramuscularly, and due to the possibility of apnoea after intravenous induction this route should be reserved for cases where intubation can be achieved[2].

Uses

Anesthetic;nociception blocker

Biological Activity

A neurosteroid anesthetic that directly activates and potentiates GABA A receptor-activated membrane current (I GABA ). Efficacy but not potency is determined by the alpha subunit of the receptor (EC 50 values are 1.4, 1.8, 2.1, 2.4 and 2.5 μ M for α 1 β 1 γ 3, α 1 β 1 γ 1, β 1 γ 1, α 2 β 1 γ 2L and α 1 β 1 γ 2L isoforms respectively).

Mechanism of action

Alfaxalone's mechanism of action is chloride ion modulation associated with interaction with the neuronal membrane GABA A receptor[1].

Side effects

Alfaxalone is safe and effective at 12–15 mg/kg IM for routine noninvasive procedures and lasts approximately 40–45 min. The most common side effects are dose-dependent but transient hypotension (15 min), hypoventilation, and apnea. Higher doses of alfaxalone (12 mg/kg) may cause mild hypoxemia, which can be corrected by administration of supplemental oxygen via face mask. Muscle twitching occurs toward the end of immobilization and can be used as a sign of impending emergence[1].

References

[1] Marini, R. and J. Haupt. “Anesthesia and Select Surgical Procedures.” The Common Marmoset in Captivity and Biomedical Research 61 1 (2019).
[2] Molly Varga BVetMed DZooMed MRCVS. “Anaesthesia and Analgesia.” Textbook of Rabbit Medicine (Second Edition) (2014): 178-202.

Alfaxalone Preparation Products And Raw materials

Alfaxalone Suppliers

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Zhejiang J&C Biological Technology Co.,Limited +1-2135480471 +1-2135480471 China 10522 58 Inquiry
3ALPHA-HYDROXY-5ALPHA-PREGNANE-11,20-DIONE 3-HYDROXY-5ALPHA-PREGNANE-11,20-DIONE 5ALPHA-PREGNAN-3ALPHA-OL-11,20-DIONE ALFAXALONE ALPHAXALONE (3-alpha,5-alpha)-3-hydroxypregnane-11,20-dione 20-dione,3-alpha-hydroxy-5-alpha-pregnane-1 20-dione,3-hydroxy-,(3-alpha,5-alpha)-pregnane-1 3-hydroxypregnane-11,20-dione gr2/234 5A-pregnan-3A-ol-11,20-dione Pregnane-11,20-dione, 3-hydroxy-, (3.alpha.,5.alpha.)- 3-Hydroxy-5α-pregnane-11,20-dione, Alfaxalone 5α-Pregnan-3α-ol-11,20-dione 3α-Hydroxy-5α-pregnane-11,12-dione (3α,5α)-3-Hydroxypregnane-11,20-dione Pregnane-11,20-dione,3-hydroxy-, (3a,5a)- Alphaxolone Pregnane-11,20-dione, 3-hydroxy-, (3α,5α)- (3R,5S,8S,9S,10S,13S,14S,17S)-17-acetyl-3-hydroxy-10,13-dimethyltetradecahydro-1H-cyclopenta[a]phenanthren-11(2H)-one ALFAXALONE USP/EP/BP (3α,5α)-3-Hydroxypregnane-11,20-dione 5α-PREGNAN-3α-OL-11, 20-DIONE 23930-19-0 GABA and Glycine Receptor Modulators Ion Channels Ligand-Gated Ion Channels BioChemical Cell Signaling and Neuroscience Cell Biology