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Chemistry

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Also known as: Ivermectin, Dihydroavermectin b1a, 70288-86-7, 22,23-dihydroavermectin b1a, 70161-11-4, Ivermectin component b1a
Molecular Formula
C48H74O14
Molecular Weight
875.1  g/mol
InChI Key
AZSNMRSAGSSBNP-XPNPUAGNSA-N
FDA UNII
91Y2202OUW

Ivermectin
A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form.
1 2D Structure

Ivermectin

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
2.1.2 InChI
InChI=1S/C48H74O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+/m0/s1
2.1.3 InChI Key
AZSNMRSAGSSBNP-XPNPUAGNSA-N
2.1.4 Canonical SMILES
CCC(C)C1C(CCC2(O1)CC3CC(O2)CC=C(C(C(C=CC=C4COC5C4(C(C=C(C5O)C)C(=O)O3)O)C)OC6CC(C(C(O6)C)OC7CC(C(C(O7)C)O)OC)OC)C)C
2.1.5 Isomeric SMILES
CC[C@H](C)[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
2.2 Other Identifiers
2.2.1 UNII
91Y2202OUW
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Eqvalan

2. Ivermectin

3. Ivomec

4. Mectizan

5. Mk 933

6. Mk-933

7. Mk933

8. Stromectol

2.3.2 Depositor-Supplied Synonyms

1. Ivermectin

2. Dihydroavermectin B1a

3. 70288-86-7

4. 22,23-dihydroavermectin B1a

5. 70161-11-4

6. Ivermectin Component B1a

7. 71827-03-7

8. Avermectin H2b1a

9. 5-o-demethyl-22,23-dihydroavermectin A1a

10. Chebi:63941

11. 91y2202ouw

12. (2ae,4e,5's,6s,6'r,7s,8e,11r,13r,15s,17ar,20r,20ar,20bs)-6'-[(2s)-butan-2-yl]-20,20b-dihydroxy-5',6,8,19-tetramethyl-17-oxo-3',4',5',6,6',10,11,14,15,17,17a,20,20a,20b-tetradecahydro-2h,7h-spiro[11,15-methanofuro[4,3,2-pq][2,6]benzodioxacyclooctadecine-13,2'-pyran]-7-yl 2,6-dideoxy-4-o-(2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)-3-o-methyl-alpha-l-arabino-hexopyranoside

13. Mk-933

14. (1r,4s,5's,6r,6'r,8r,10e,12s,13s,14e,16e,20r,21r,24s)-6'-[(2s)-butan-2-yl]-21,24-dihydroxy-12-[(2r,4s,5s,6s)-5-[(2s,4s,5s,6s)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one

15. Ivermectin B1a-d2

16. C48h74o14

17. Unii-91y2202ouw

18. 22,23-dihydroavermectin B(1)a

19. Ncgc00163233-01

20. Ivermectin (ivm)

21. Ivm

22. Einecs 276-046-2

23. Dihydro Avermectin Bla

24. Brn 4643153

25. 22,23-dihydro-5-o-demethylavermectin A1a

26. H2b1a

27. Prestwick3_000156

28. Dsstox_cid_3181

29. Ivermectin (mk-0933)

30. Dsstox_rid_76909

31. Dsstox_gsid_23181

32. Bspbio_000292

33. Schembl312795

34. Bpbio1_000322

35. Chembl263291

36. Dtxsid8023181

37. Chebi:94551

38. Hms2089m09

39. Hms2095o14

40. Hms3712o14

41. Wca82703

42. Tox21_112034

43. Bdbm50409816

44. Mfcd30496678

45. S1351

46. Akos027470116

47. Ivermectin Component B1a [mi]

48. Zinc238808778

49. Zinc252286706

50. Ac-6014

51. Ccg-220156

52. Ncgc00186639-01

53. Ncgc00186639-03

54. As-14167

55. Bi166167

56. Cas-71827-03-7

57. Hy-126937

58. Ab00513813

59. Cs-0108408

60. 22,23-dihydroavermectin B1a; Ivermectin

61. Ab00513813-02

62. Ab00513813-03

63. Ab00513813_04

64. Avermectin A1a, 22,23-dihydro-5-o-demethyl-

65. 288i867

66. Ivermectin, Antibiotic For Culture Media Use Only

67. Q-201262

68. Brd-k24652731-001-02-7

69. Brd-k85554912-001-08-9

70. Q27132923

71. Ivermectin, British Pharmacopoeia (bp) Reference Standard

72. Ivermectin, European Pharmacopoeia (ep) Reference Standard

73. Ivermectin, United States Pharmacopeia (usp) Reference Standard

74. Ivermectin, Pharmaceutical Secondary Standard; Certified Reference Material

75. (2ae,4e,5's,6s,6'r,7s,8e,11r,13r,15s,17ar,20r,20ar,20bs)-6'-[(2s)-butan-2-yl]-20,20b-dihydroxy-5',6,8,19-tetramethyl-17

76. Clooctadecine-13,2'-pyran]-7-yl 2,6-dideoxy-4-o-(2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)-3-o-methyl-alpha-l-arabino-hexopyranoside

2.4 Create Date
2005-11-20
3 Chemical and Physical Properties
Molecular Weight 875.1 g/mol
Molecular Formula C48H74O14
XLogP34.1
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count14
Rotatable Bond Count8
Exact Mass874.50785703 g/mol
Monoisotopic Mass874.50785703 g/mol
Topological Polar Surface Area170 Ų
Heavy Atom Count62
Formal Charge0
Complexity1680
Isotope Atom Count0
Defined Atom Stereocenter Count20
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count3
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Treatment of rosacea


5 Pharmacology and Biochemistry
5.1 MeSH Pharmacological Classification

Antiparasitic Agents

Drugs used to treat or prevent parasitic infections. (See all compounds classified as Antiparasitic Agents.)


Insecticides

Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics. (See all compounds classified as Insecticides.)


5.2 FDA Pharmacological Classification
5.2.1 Pharmacological Classes
Pediculicide [EPC]; Antiparasitic [EPC]
5.3 ATC Code

D - Dermatologicals

D11 - Other dermatological preparations

D11A - Other dermatological preparations

D11AX - Other dermatologicals

D11AX22 - Ivermectin


P - Antiparasitic products, insecticides and repellents

P02 - Anthelmintics

P02C - Antinematodal agents

P02CF - Avermectines

P02CF01 - Ivermectin


API Reference Price

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14-Jan-2021
29-Nov-2024
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DOSAGE - LOTION;TOPICAL - 0.5%

USFDA APPLICATION NUMBER - 202736

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DOSAGE - CREAM;TOPICAL - 1%

USFDA APPLICATION NUMBER - 206255

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