CAS 70288-86-7|Ivermectin

Introduction：Basic information about CAS 70288-86-7|Ivermectin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Ivermectin BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles99
8. Synonyms

Common Name	Ivermectin
CAS Number	70288-86-7	Molecular Weight	875.09300
Density	/	Boiling Point	/
Molecular Formula	C₄₈H₇₄O₁₄	Melting Point	155 °C
MSDS	ChineseUSA	Flash Point	/
Symbol	GHS06	Signal Word	Danger

Names

Name	ivermectin
Synonym	More Synonyms

Ivermectin BiologicalActivity

Description	Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
Related Catalog	Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Autophagy >>MitophagySignaling Pathways >>Anti-infection >>ParasiteResearch Areas >>Infection
In Vitro	Ivermectin (IVM) is a specific positive allosteric effector of heterologously expressed P2X4 and possibly of heteromeric P2X4/ P2X6 channels. In the submicromolar range (EC50=250 nM) the action of IVM is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4 channel currents evoked by ATP. IVM also markedly increases the potency of ATP and that of the normally low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X4 channels[1]. IVM activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis. The major mode of action of IVM is most likely the disruption of ingestive activity of the parasite, resulting in starvation[2]. Preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human α7 nicotinic acetylcholine receptors reconstituted in Xenopus laevis oocytes and K-28 cells[3]. Ivermectin activates the rat recombinant α1β2γ2s GABAA receptor. Activation of the channel with 10 mM GABA results in currents rising within 1 ms to their maximal amplitudes. The EC50 value for GABA is 7.5 μM[4].
References	[1]. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999 Sep 1;19(17):7289-99. [2]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93. [3]. Krause RM, et al. Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor. Mol Pharmacol. 1998 Feb;53(2):283-94. [4]. Adelsberger H, et al. Activation of rat recombinant alpha(1)beta(2)gamma(2S) GABA(A) receptor by the insecticide ivermectin. Eur J Pharmacol. 2000 Apr 14;394(2-3):163-70.

Chemical & Physical Properties

Melting Point	155 °C
Molecular Formula	C₄₈H₇₄O₁₄
Molecular Weight	875.09300
Exact Mass	874.50800
PSA	170.06000
LogP	5.60140
InChIKey	AZSNMRSAGSSBNP-ONDMGMIHSA-N
SMILES	CCC(C)C1OC2(CCC1C)CC1CC(CC=C(C)C(OC3CC(OC)C(OC4CC(OC)C(O)C(C)O4)C(C)O3)C(C)C=CC=C3COC4C(O)C(C)=CC(C(=O)O1)C34O)O2
Storage condition	2-8°C
Water Solubility	H2O: ≤1.0% KF

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: IH7891500

CHEMICAL NAME :: 22,23-Dihydroavermectin B1

CAS REGISTRY NUMBER :: 70288-86-7

LAST UPDATED :: 199309

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 29500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AJVRAH American Journal of Veterinary Research. (American Veterinary Medical Assoc., 930 N. Meacham Rd., Schaumburg, IL 60196) V.1- 1940- Volume(issue)/page/year: 53,2032,1992

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cattle

DOSE/DURATION :: 8 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: SCIEAS Science. (American Assoc. for the Advancement of Science, 1333 H St., NW, Washington, DC 20005) V.1- 1895- Volume(issue)/page/year: 221,823,1983 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 73 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 27,523,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 655 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - other postnatal measures or effects

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 27,523,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 72 mg/kg

SEX/DURATION :: female 6-20 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 10,267,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 mg/kg

SEX/DURATION :: female 6-20 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

REFERENCE :: NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 10,267,1988

Safety Information

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H300
Precautionary Statements	Missing Phrase - N15.00950417
Personal Protective Equipment	Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes	T: Toxic;
Risk Phrases	61-25-36-36/38-22
Safety Phrases	53-26-45-36
RIDADR	UN 2811 6.1/PG 2
WGK Germany	3
Packaging Group	II
Hazard Class	6.1(a)
HS Code	2932999099

Customs

HS Code	2932999099
Summary	2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles99

Permethrin and ivermectin for scabies.

N. Engl. J. Med. 362(8) , 717-25, (2010)

Cytokine responses to egg protein in previously allergic children who developed tolerance naturally.

Ann. Allergy Asthma Immunol. 113(6) , 667-670.e4, (2014)

[Comparative activity of different groups of insecticides against permethrin-resistant lice (anoplura: pediculidae)].

Med. Parazitol. (Mosk.) (1) , 20-7, (2013)

The activity of insecticides (CK50, CK95 ) from different chemical classes against permethrin-resistant body and head lice was investigated. Having developed resistance to pyrethroids (permethrin, d-p...

Synonyms

Vermic

mk933

Ivosint

EINECS 274-536-0

22,23-dihydroavermectin B1

MFCD00869511

(1'R,2R,4'S,5S,6R,8'R,10'E,12'S,13'S,14'E,16'E,20'R,21'R,24'S)-21',24'-dihydroxy-12'-{[(2R,4S,5S,6S)-5-{[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-4-methoxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-5,11',13',22'-tetramethyl-6-[(1S)-1-methylpropyl]-3,4,5,6-tetrahydro-2'H-spiro[pyran-2,6'-[3,7,19]trioxatetracyclo[15.6.1.1.0]pentacosa[10,14,16,22]tetraen]-2'-one

Mectizan

mk-0933

CARDOMEC

IVOMEC

Ivermecti

Uvemec

Ivermectin

EQVALEN

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