子囊霉素(他克莫司相关化合物A)
Ascomycin
CAS: 104987-12-4;11011-38-4
Molecular Formula: C43 H69 N O12
子囊霉素(他克莫司相关化合物A) - Names and Identifiers
子囊霉素(他克莫司相关化合物A) - Physico-chemical Properties
| Molecular Formula | C43 H69 N O12 |
| Molar Mass | 792.01 |
| Density | 1.19±0.1 g/cm3(Predicted) |
| Melting Point | 153-157°C |
| Boling Point | 868℃ |
| Flash Point | >110°(230°F) |
| Water Solubility | Soluble in DMSO at 65mg/ml; soluble in ethanol at 50mg/m; with warming. Very poorly soluble in water |
| Solubility | Soluble in methanol, ethanol, DMSO and other organic solvents |
| Appearance | White powder |
| pKa | 9.97±0.70(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.543 |
| Physical and Chemical Properties | Storage Conditions:? 20℃ WGK Germany:3 RTECS:KD4185000 |
| In vitro study | Ascomectin, isolated from Streptomyces, inhibits the in vitro immune response of mouse mixed lymphocytes with an IC50 of 0.55 nM. Ascomectin inhibits calcineurin by FKBP12-FK520 the formation of the calcineurin ternary complex with an IC50 of 49 nM. FK520 also accelerates the rate of nerve repair and also promotes neurite outgrowth. Ascomcin exhibits an antimalarial effect by inhibiting the chaperone activity of two different functional proteins. |
| In vivo study | Ascomectin (3.2 mg/kg, intramuscular injection) significantly prolonged the survival rate of skin graft rats. Ascomectin, at 50 or 100 μm, exerted a resistant effect on the spasm induced by picrotoxin injected into the rat hippocampus. |
子囊霉素(他克莫司相关化合物A) - Risk and Safety
| Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36 - Irritating to the eyes R11 - Highly Flammable |
| Safety Description | S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. |
| UN IDs | UN 1648 3 / PGII |
| WGK Germany | 3 |
| RTECS | KD4185000 |
| FLUKA BRAND F CODES | 10 |
| HS Code | 29419090 |
子囊霉素(他克莫司相关化合物A) - Reference
| Reference Show more | 1. Yue Xiujuan and Wang Yongmei. Determination of Sirolimus in Whole Blood by HPLC-MS/MS [J]. China 2013 for Drug Application and Monitoring (4):206-208. 2. [IF = 4.36] Xiangling Feng et al."Inhibitory effects of traditional Chinese medicine colquhounia root tablet on the pharmacokinetics of tacrolimus in rats." JOURNAL OF ETHNOPHARMACOLOGY. 2022 Aug;294:115358 |
子囊霉素(他克莫司相关化合物A) - Nature
Open Data Verified Data
- The original changchuanmycin (content ≥ 94%) was white to light yellow powder in appearance, without visible foreign impurities. Melting Point: 163~164 ℃; Solubility: soluble in methanol, ethanol, acetone, ethyl acetate, chloroform, slightly soluble in hexane, petroleum ether, insoluble in water; Stability: stable in organic solvents, tautomers are formed in an aqueous medium.
- formulation 1% changchuanmycin emulsifiable concentrate.
Last Update：2024-01-02 23:10:35
子囊霉素(他克莫司相关化合物A) - Preparation Method
Open Data Verified Data
The microorganism producing changchuanmycin is a strain belonging to the genus Streptomyces, which was isolated from the soil in Wuzhou area of Guangxi, China by the Shanghai Institute of pesticides, the strain was named Streptomyces nigrosporum Guangxi variant (Steptomyces melan,osporo faciens var.guanxicus spri 520).
Last Update：2022-01-01 11:18:56
子囊霉素(他克莫司相关化合物A) - Use
Open Data Verified Data
changchuanmycin is a microbial source of fungicides, with root absorption, but no leaf absorption conduction. It inhibited the spore germination and mycelial growth of Botrytis cinerea. The field efficacy test showed that it had good control effect on tomato gray mold, the dosage (active ingredient) was 75~112.5g/hm2, diluted with water, usually added water 75kg, after mixing evenly foliar spray. The use period is the early stage of the disease of tomato gray mold (tomato in a tower flowering fruit period), generally continuous spraying 2~6 times, depending on the disease, the interval of 7d spraying 1 time. Laboratory tests found that changchuanmycin on maize leaf blight, rice blast, anthracnose, powdery mildew, Sclerotinia sclerotiorum, downy mildew and other crop fungal diseases also have good control effect.
Last Update：2022-01-01 11:18:57
子囊霉素(他克莫司相关化合物A) - Safety
Open Data Verified Data
The original drug of changchuanmycin is moderately toxic, acute oral LD50 in rats, male 270mg/kg, female 126 mg/kg; Acute percutaneous LD50>2000mg/kg in rats; no irritation to rabbit skin, rabbit eyes mild irritation; Guinea pig skin sensitization test results are moderate sensitization; Rats 90d subchronic feeding test maximum non-effective dose of male 6. 5mg.kg-1.d-1, female 1. 3mg.kg-1.d-1; Mutagenicity test: Ames test, mouse bone marrow cell micronucleus test and mouse testicular cell chromosome aberration test were all negative. 1% changchuanmycin EC is a low toxicity fungicide, rats acute oral LD50 male 2000mg/kg, female 1080mg/kg; Rats acute percutaneous LD50>2000mg/kg; the results of skin sensitization test on rabbits were weak sensitizers; 1% changchuanmycin EC on zebrafish LC50(48h)1.35mg/L; Bee LC50 (stomach poison method, 48h) 271. 08mg/L; Quail LD50 (direct oral injection, 7d)15. 2 mg/kg; Silkworm with unit mass of mulberry leaf LD50 (food poison leaf method, 2) 2065mg/kg. 1% of changchuanmycin emulsifiable concentrate for fish and birds for moderate toxicity, for medium risk to bees, for low risk of silkworm. Pay attention to the use of fish, birds, bees.
Last Update：2022-01-01 11:18:57
子囊霉素(他克莫司相关化合物A) - Reference Information
| agricultural antibiotic | changchuan mycin is a macrolide agricultural antibiotic independently created and developed by Shanghai Institute of Pesticides. It is a biological pesticide and can effectively control tomato gray mold, Cucumber gray mold, corn spot and other fungal diseases of crops. China has historically approved the following four Changchuanmycin products for temporary registration, but as of the end of June 2019, none of them have been transferred to official registration. Therefore, according to the relevant provisions of the "Pesticide Management Regulations", the changchuan mycin products currently sold on the market in my country are all fake pesticides. |
| use | the fungicide has good control effect on cucumber gray mold, corn spot disease, sclerotinia sclerotiorum, powdery mildew and other fungal diseases, can be widely used in strawberry, tomato, cucumber and other cash crops, and can replace carbendazim, thiophanate methyl, sukeling and other pesticides with serious resistance. |
| biological activity | Ascomycin (FK520, FR 900520, Immunomycin), a FK-506 analog, is a neutral macrolide immunosuppressant that can prevent rejection after organ transplantation. |
| Target | Value |
| calcineurin phosphatase | 49 nM |
Last Update：2024-04-09 20:52:54
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View History
子囊霉素(他克莫司相关化合物A)
Methanone, (3'-nitro[1,1'-biphenyl]-4-yl)phenyl-
酸性蓝3号钠盐,酸性蓝3号
DIETHYL ACETAMIDOMALONATE-2-13C
2,3,4,5-tetramethyl-2-cyclopentanone (cis+trans)
MAGNESIUM MONOPEROXYPHTHALATE HEXAHYDRATE
4-METHYLVALERYL CHLORIDE
Methanone, (3'-nitro[1,1'-biphenyl]-4-yl)phenyl-
酸性蓝3号钠盐,酸性蓝3号
DIETHYL ACETAMIDOMALONATE-2-13C
2,3,4,5-tetramethyl-2-cyclopentanone (cis+trans)
MAGNESIUM MONOPEROXYPHTHALATE HEXAHYDRATE
4-METHYLVALERYL CHLORIDE