Drug
D0434 | rapamycin
S
L
S01XA23 Sirolimus
[S01XA] Other ophthalmologicals
[S01X] OTHER OPHTHALMOLOGICALS
[S01] OPHTHALMOLOGICALS
[S] Sensory organs
L04AA10 Sirolimus
[L04AA] Selective immunosuppressants
[L04A] IMMUNOSUPPRESSANTS
[L04] IMMUNOSUPPRESSANTS
[L] Antineoplastic and immunomodulating agents
| Toxicity | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| MEMBRANE POTENTIAL | 20.08±2.07 | human | qHTS-HepG2 | MMP assay | decrease | IC50 | 163 | |
| MEMBRANE POTENTIAL | 20.64±1.68 | rat | hepatocytes | MMP assay | decrease | IC50 | 163 | |
| RESPIRATORY CONTROL RATIO (RCR) | 1 μM | rat | isolated kidney mitochondria | Oxygen consumption was measured with a Clark‐type electrode | decrease | 11% | 323 | |
| RESPIRATORY CONTROL RATIO (RCR) | 4.4×10−10 M | rat | isolated kidney mitochondria | Oxygen consumption was measured with a Clark‐type electrode | decrease | EC50 ; maximal inhibitory effect was about14% | 323 | |
| P/O RATIO ( ADP/O) | 1 μM | rat | isolated kidney mitochondria | Oxygen consumption was measured with a Clark‐type electrode | decrease | 323 | ||
| TRANSPORT OF CALCIUM | 1 μM | rat | isolated kidney mitochondria | Ca2+ fluxes: A specific Ca2+ electrode (Orion 9320) fitted to a Hansatech recorder via a 720A Orion ionometer was used to record Ca2+ movements in extramitochondrial medium in a thermostat‐controlled reaction chamber. | Negative | 323 | ||
| SWELLING | 1 μM | rat | isolated kidney mitochondria | Measurement of swelling of energized mitochondria: measuring the decrease of optical density at 520 nm, with a Hitachi spectrophotometer (U3000) | Negative | 323 | ||
| MITOPHAGY | mouse | embryonic retinas | Mitochondrial population levels were determined by flow cytometry using MitoTracker Deep Red (MTDR) dye | 252 | ||||
| CYTOCHROME C RELEASE | 1 μM | rat | isolated kidney mitochondria | The amount of cytochrome c was measured using a Quantikine® M Rat/Mouse Cytochrome c immunoassay after addition of drugs in energized mitochondrial (3 min) or after Ca2+‐induced mitochondrial swelling (3 min). | Negative | 323 | ||
| SIGNALING | 200 nM | 252 | ||||||
| Target | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| Quinol--cytochrome-c reductase | 1 μM | rat | isolated kidney mitochondria | Mitochondrial complex III assay (ubiquinol‐cytochrome c oxidoreductase) | inhibit | 24% | 323 | |
| Serine/threonine-protein kinase mTOR | mouse | embryonic retinas | Mitochondrial population levels were determined by flow cytometry using MitoTracker Deep Red (MTDR) dye | 252 | ||||
| Serine/threonine-protein kinase mTOR | 200 nM | 252 | ||||||
| Pictogram | Signal | Statements | Precautionary Statement Codes |
|---|---|---|---|
 |
Danger |
Aggregated GHS information provided by 165 companies from 10 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. H351 (96.36%): Suspected of causing cancer [Warning Carcinogenicity] H361 (97.58%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity] H372 (96.36%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure] Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. |
P201, P202, P260, P264, P270, P281, P308+P313, P314, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| (-)-Rapamycin | (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-Dihydroxy-12-{(2S)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone | (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-{(2S)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0(4,9)]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone |
| (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34 aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hex adecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydro xy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy- 6,8,12,14,20,26-hexamethyl-23,27-ep | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-4,9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-heptadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-223,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(6H,31H)-pentone | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-((1R)-2-((1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl)-1-methylethyl)-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone |
| (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-hydroxy-3-(methyloxy)cyclohexyl]-1-methylethyl}-6,8,12,14,20,26-hexamethyl-10,21-bis(methyloxy)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-hydroxy-3-(methyloxy)cyclohexyl]-1-methylethyl}-6,8,12,14,20,26-hexamethyl-10,21-bis(methyloxy)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(6H,31H)-pentone | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone |
| (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23, | 1,18-Dihydroxy-12-[2-(4-hydroxy-3-methoxy-cyclohexyl)-1-methyl-ethyl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-aza-tricyclo[30.3.1.0*4,9*]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentaone (Rapamycin); |
| 123R889 | 1fkb | 1pbk |
| 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine | 24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypy | 53123-88-9 |
| A-275 | AC-722 | ACN-035837 |
| AKOS015850976 | AKOS015961618 | AS-11687 |
| AY 22989 | AY 22989 pound notNSC-2260804 | AY-22989 |
| Antibiotic AY 22989 | BDBM36609 | BDBM50064359 |
| BIDD:PXR0165 | BRD-K84937637-001-04-0 | BRD-K84937637-001-06-5 |
| BRD-K89626439-001-01-0 | BiomolKI2_000084 | C51H79NO13 |
| CAS-53123-88-9 | CCG-100684 | CCRIS 9024 |
| CHEBI:9168 | CS-0063 | Cypher |
| DB00877 | DE-109 | DSSTox_CID_3582 |
| DSSTox_GSID_23582 | DSSTox_RID_77091 | DTXSID5023582 |
| EC 610-965-5 | EX-A1044 | FT-0082351 |
| GTPL6031 | HMS2089A21 | HMS3403F11 |
| HSDB 7284 | HY-10219 | L04AA10 |
| LCP-Siro | LS-143290 | MFCD00867594 |
| MLS006010168 | MS-R001 | NCGC00021305-05 |
| NCGC00021305-06 | NCGC00021305-07 | NCGC00181146-01 |
| NSC 226080 | NSC-226080 | NSC-2260804 |
| NSC226080 | Perceiva | PubChem16645 |
| Q-201659 | Q32089 | QFJCIRLUMZQUOT-HPLJOQBZSA-N |
| R0097 | RAP | RAPA |
| Rapammune | Rapamune | Rapamycin |
| Rapamycin (Sirolimus) | Rapamycin C-7, analog 4 | Rapamycin from Streptomyces hygroscopicus, >=95% (HPLC), powder |
| Rapamycin from Streptomyces hygroscopicus, Vetec(TM) reagent grade, >=95% | Rapamycin, VETRANAL(TM), analytical standard | Rapamycin,Sirolimus,Rapamune |
| S-7759 | S1039 | SCHEMBL3463 |
| SILA 9268A | SM-88 COMPONENT SIROLIMUS | SMR004701276 |
| STL570275 | SYN1185 | Sirolimus |
| Sirolimus (RAPAMUNE) | Sirolimus [USAN:BAN:INN] | Sirolimus [USAN:INN:BAN] |
| Sirolimus solution, 1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material | Supralimus | Tox21_110870 |
| Tox21_112750 | UNII-W36ZG6FT64 | UNM-0000358684 |
| W36ZG6FT64 | WY-090217 | Wy 090217 |
| ZINC169289388 | sirolimusum |