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1492-18-8

1492-18-8 structure
1492-18-8 structure
  • Name: Folinic acid (Calcium)
  • Chemical Name: Folinic acid calcium salt hydrate
  • CAS Number: 1492-18-8
  • Molecular Formula: C20H21CaN7O7
  • Molecular Weight: 511.501
  • Catalog: API Vitamins and minerals Vitamin C drugs
  • Create Date: 2018-09-11 10:02:25
  • Modify Date: 2024-01-02 22:15:30
  • Leucovorin Calcium is a reduced folic acid.IC50 Value: 30 μM for zcSHMT and70 μM for zmSHMT [2]Target: Antifolatein vitro: Increasing concentrations of leucovorin (N5-CHO-THF) inhibit both zcSHMT and hcSHMT activities substantially, yet to a lesser extent than zmSHMT. The IC50 of leucovorin is approximately 30 μM for zcSHMT and higher than 70 μM for zmSHMT. The differential inhibition is evident with the presence of 10 μM leucovorin, the concentration estimated in serum in a high-dose leucovorin rescue regimen [2].in vivo: Following intravenous administration, peak plasma concentrations of (6R) LV, (6S) LV, and 5-CH3 THF were 148 +/- 32, 59.1 +/- 22, and 17.8 +/- 17 microM, respectively. During oral administration of LV, virtually no (6S) LV appeared in the plasma. Steady-state plasma concentrations of (6R) LV and 5-CH3 THF were approximately 1.5 +/- 0.23 and 2.8 +/- 0.41 microM, respectively [1]. 24 fasted subjects were given 4 of a series of 5 single test doses between 20 and 100 mg, at 1-week intervals, of 5-formyl-THF as an oral solution of leucovorin calcium. Six separate subjects received 200 mg iv and po in a 2-way crossover. Blood and urine samples were collected over 24 hours for differential microbiological folate assays using Lactobacillus casei and Streptococcus faecalis. Using L casei activity to measure total serum folates, the area under the concentration-time curve from 0 to infinite time (AUC[0-infinity]) was calculated. Relative bioavailabilities were 78%, 62%, 49%, and 42% for the 40-, 60-, 80-, and 100-mg doses, respectively [3].Clinical trial: Leucovorin and Fluorouracil With or Without SU-5416 in Treating Patients With Metastatic Colorectal Cancer . Phase 3

Name Folinic acid calcium salt hydrate
Synonyms L-N-(p-(((2-Amino-5-formyl-5,6,7,8-tetrahydro-3-hydroxy-6-pteridinyl)methyl)amino)benzoyl)glutamic Acid Calcium Salt (1:1)
calcium, [L-glutamato(2-)-κO,κO, N-[4-[[(2-amino-5-formyl-5,6,7,8-tetrahydro-4-hydroxy-6-pteridinyl)methyl]amino]benzoyl]-]-
(2S)-2-{[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydroptéridin-6-yl)méthyl]amino}phényl)carbonyl]amino}pentanedioate de calcium
[N-(4-{[(2-Amino-5-formyl-4-hydroxy-5,6,7,8-tetrahydropteridin-6-yl)methyl]amino}benzoyl)-L-glutamato(2-)-κO,O]calcium
5-Formyl-5,6,7,8-tetrahydropteroyl-L-glutamic acid calcium salt
Calcium folinate
5-HCO-H4PteGlu
Leucovorin calcium salt
Calcium (2S)-2-[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}benzoyl)amino]pentanedioate
MFCD00006704
Calcium-(2S)-2-{[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}phenyl)carbonyl]amino}pentandioat
Calcium Folinate Hydrate
5-Formyl-5,6,7,8-tetrahydrofolic acid calcium salt
Folinic Acid Calcium Salt Hydrate
Calcium (2S)-2-[(4-{[(2-amino-5-formyl-4-hydroxy-5,6,7,8-tetrahydropteridin-6-yl)methyl]amino}benzoyl)amino]pentanedioate
Leucovorin calcium
Calcium (2S)-2-[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydro-6-pteridinyl)methyl]amino}benzoyl)amino]pentanedioate
[N-(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}benzoyl)-L-glutamato(2-)-κO,O]calcium
EINECS 216-082-8
Folinic acid calcium salt
calcium (2S)-2-{[(4-{[(2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}phenyl)carbonyl]amino}pentanedioate
(+)-L-Folinic Acid Calcium Salt
Citrovorum factor calcium salt
L-Glutamic acid, N-[4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-, calcium salt (1:1)
calcium, [L-glutamato(2-)-κO,κO, N-[4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-]-
[N-(4-{[(2-Amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl]amino}benzoyl)-D-glutamato(2-)-κO,O]calcium
Folinic acid (Calcium)
Description Leucovorin Calcium is a reduced folic acid.IC50 Value: 30 μM for zcSHMT and70 μM for zmSHMT [2]Target: Antifolatein vitro: Increasing concentrations of leucovorin (N5-CHO-THF) inhibit both zcSHMT and hcSHMT activities substantially, yet to a lesser extent than zmSHMT. The IC50 of leucovorin is approximately 30 μM for zcSHMT and higher than 70 μM for zmSHMT. The differential inhibition is evident with the presence of 10 μM leucovorin, the concentration estimated in serum in a high-dose leucovorin rescue regimen [2].in vivo: Following intravenous administration, peak plasma concentrations of (6R) LV, (6S) LV, and 5-CH3 THF were 148 +/- 32, 59.1 +/- 22, and 17.8 +/- 17 microM, respectively. During oral administration of LV, virtually no (6S) LV appeared in the plasma. Steady-state plasma concentrations of (6R) LV and 5-CH3 THF were approximately 1.5 +/- 0.23 and 2.8 +/- 0.41 microM, respectively [1]. 24 fasted subjects were given 4 of a series of 5 single test doses between 20 and 100 mg, at 1-week intervals, of 5-formyl-THF as an oral solution of leucovorin calcium. Six separate subjects received 200 mg iv and po in a 2-way crossover. Blood and urine samples were collected over 24 hours for differential microbiological folate assays using Lactobacillus casei and Streptococcus faecalis. Using L casei activity to measure total serum folates, the area under the concentration-time curve from 0 to infinite time (AUC[0-infinity]) was calculated. Relative bioavailabilities were 78%, 62%, 49%, and 42% for the 40-, 60-, 80-, and 100-mg doses, respectively [3].Clinical trial: Leucovorin and Fluorouracil With or Without SU-5416 in Treating Patients With Metastatic Colorectal Cancer . Phase 3
Related Catalog
References

[1]. Schilsky RL, Ratain MJ. Clinical pharmacokinetics of high-dose leucovorin calcium after intravenous and oral administration. J Natl Cancer Inst. 1990 Sep 5;82(17):1411-5.

[2]. Chang WN, Tsai JN, Chen BH, Serine hydroxymethyltransferase isoforms are differentially inhibited by leucovorin: characterization and comparison of recombinant zebrafish serine hydroxymethyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2127-37.

[3]. McGuire BW, Sia LL, Haynes JD, Absorption kinetics of orally administered leucovorin calcium. NCI Monogr. 1987;(5):47-56.

Melting Point 240-250ºC
Molecular Formula C20H21CaN7O7
Molecular Weight 511.501
Exact Mass 511.112823
PSA 198.10000
LogP 1.41100

CHEMICAL IDENTIFICATION

RTECS NUMBER :
MA0600500
CAS REGISTRY NUMBER :
1492-18-8
LAST UPDATED :
199706
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C20-H21-N7-O7.Ca
MOLECULAR WEIGHT :
511.56
WISWESSER LINE NOTATION :
T66 BN DN GN JM&TJ CZ EQ GVH I1MR DVMYVO2VO &-NA-

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 :
>8 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: 23,93,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1063 mg/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: 23,93,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>7 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: 23,93,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1036 mg/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: 23,93,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
732 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,910,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6060 No. of Facilities: 103 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 3686 (estimated) No. of Female Employees: 2084 (estimated)
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Danger
Hazard Statements H315-H317-H319-H334-H335
Precautionary Statements P261-P280-P305 + P351 + P338-P342 + P311
Hazard Codes Xn:Harmful
Risk Phrases R36/37/38;R42/43
Safety Phrases S26-S36-S36/37-S22
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS MA0600500
HS Code 2942000000
Precursor  1

DownStream  0

HS Code 2942000000