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China
Product Name: Repirinast
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Purity: 98.0%
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Contact: Tony Cao

73080-51-0

73080-51-0 structure

Name: Repirinast
Chemical Name: 3-methylbutyl 7,8-dimethyl-4,5-dioxo-6H-pyrano[3,2-c]quinoline-2-carboxylate
CAS Number: 73080-51-0
Molecular Formula: C₈H₁₁N₇O
Molecular Weight: 221.219
Catalog: API Respiratory medication Asthma
Create Date: 2018-08-19 11:12:15
Modify Date: 2024-01-02 13:23:27
Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma[1][2][3].

Name	3-methylbutyl 7,8-dimethyl-4,5-dioxo-6H-pyrano[3,2-c]quinoline-2-carboxylate
Synonyms	Isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano(3,2-c)quinoline-2-carboxylate MY-5116 Repirinastum [INN-Latin] Diazenecarboxamide, 2-[4-[2-(diaminomethylene)hydrazinyl]phenyl]-, (E)- Romet Isopentyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano(3,2-c)quinoline-2-carboxylate (E)-2-{4-[2-(Diaminomethylene)hydrazino]phenyl}diazenecarboxamide repirinast

Description	Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma[1][2][3].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Inflammation/Immunology
In Vitro	Repirinast inhibits histamine release from rat peritoneal mast cells induced by antigen (IC50: 0.3 μM)[3].
In Vivo	Repirinast (30 mg/kg, i.p.) inhibits antigen-induced early and late pulmonary responses in guinea pigs[1]. Repirinast (30 mg/kg, p.o.) inhibits antigen-induced immediate bronchoconstriction in rats[2]. Animal Model: Guinea pigs[1] Dosage: 30 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Inhibited leukocyte (predominantly eosinophils) infiltration into bronchial tissue. Blocked antigen-induced airway hyperresponsiveness to inhaled Acetylcholine. Animal Model: Rat with asthma (challenged with 10 mg/kg antigen OVA)[1] Dosage: 30 mg/kg Administration: Oral administration (p.o.) Result: Inhibited the decreases in the number Of breath at 30 sec and 1 min after challenge.
References	[1]. N Yamada, et al. Repirinast inhibits antigen-induced early and late pulmonary responses and airway hyperresponsiveness in guinea pigs. Int Arch Allergy Immunol. 1993;100(4):367-72. [2]. Takahashi K. Effects of MY-5116 on experimental asthma in rats and guinea pigs. Arerugi. 1986 Oct; 35(10): 1037-46. [3]. M Takei, et al. Inhibition of histamine release from rat peritoneal mast cells by MY-1250, an active metabolite of Repirinast (MY-5116). Int Arch Allergy Appl Immunol. 1990;93(2-3):237-41.

Density	1.6±0.1 g/cm3
Boiling Point	461.1±55.0 °C at 760 mmHg
Melting Point	236-241°
Molecular Formula	C₈H₁₁N₇O
Molecular Weight	221.219
Flash Point	232.6±31.5 °C
Exact Mass	221.102509
PSA	89.37000
LogP	0.46
Vapour Pressure	0.0±1.1 mmHg at 25°C
Index of Refraction	1.731

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ1377000

CHEMICAL NAME :: 4H-Pyrano(3,2-c)quinoline-2-carboxylic acid, 5,6-dihydro-7,8-dimethyl-4,5-dioxo-, isopentyl ester

CAS REGISTRY NUMBER :: 73080-51-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C20-H21-N-O5

MOLECULAR WEIGHT :: 355.42

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2783 mg/kg

TOXIC EFFECTS :: Gastrointestinal - peritonitis Kidney, Ureter, Bladder - other changes

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1435 mg/kg

TOXIC EFFECTS :: Gastrointestinal - peritonitis Kidney, Ureter, Bladder - other changes

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,577,1986

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - changes primarily in glomeruli Blood - changes in spleen

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,545,1986 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5200 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - abortion Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,51,1986

HS Code	2934999090

63768-46-7

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256

87-59-2

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256

63768-47-8

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256

123-51-3

73080-52-1

73080-51-0

Literature: European Journal of Medicinal Chemistry, , vol. 16, # 3 p. 251 - 256

Precursor 5
63768-46-7 87-59-2 63768-47-8 123-51-3
73080-52-1
DownStream 0

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%