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Hydroxocobalamin Sale

(Synonyms: 羟钴胺) 目录号 : GC43875

A biologically active form of Vitamin B12

Hydroxocobalamin Chemical Structure

Cas No.:13422-51-0

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5mg
¥516.00
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产品描述

Hydroxocobalamin is a biologically active form of vitamin B12 . It increases the number of red blood cells 2.5-fold over control in a mouse model of anemia when administered at a dose of 2 µg per day for 4 days. Hydroxocobalamin is also efficacious in animal models of cyanide poisoning. Formulations containing hydroxocobalamin have been used in the treatment of vitamin B12 deficiency and cyanide poisoning.

Chemical Properties

Cas No. 13422-51-0 SDF
别名 羟钴胺
Canonical SMILES [OH-][Co+3]123([N]4=CN(C(OC(CO)C5O[P]6([O-])=O)C5O)C7=C4C=C(C)C(C)=C7)[N]8=C9C(CCC(N)=O)C(CC(N)=O)(C)C8(C)C(C(CC(N)=O)C%10(CCC(NCC(C)O6)=O)C)[N-]1C%10=C(C)C(C(CCC(N)=O)C%11(C)C)=[N]2C%11=CC%12=[N]3C(C(C)(CC(N)=O)C%12CCC(N)=O)=C9C
分子式 C62H89CoN13O15P 分子量 1346.4
溶解度 Methanol: Slightly Soluble,Water: Slightly Soluble 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 0.7427 mL 3.7136 mL 7.4272 mL
5 mM 0.1485 mL 0.7427 mL 1.4854 mL
10 mM 0.0743 mL 0.3714 mL 0.7427 mL
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Research Update

Treatment of vitamin B12 deficiency-methylcobalamine? Cyancobalamine? Hydroxocobalamin?-clearing the confusion

Eur J Clin Nutr 2015 Jan;69(1):1-2.PMID:25117994DOI:10.1038/ejcn.2014.165.

Vitamin B12 (cyancobalamin, Cbl) has two active co-enzyme forms, methylcobalamin (MeCbl) and adenosylcobalamin (AdCbl). There has been a paradigm shift in the treatment of vitamin B12 deficiency such that MeCbl is being extensively used and promoted. This is despite the fact that both MeCbl and AdCbl are essential and have distinct metabolic fates and functions. MeCbl is primarily involved along with folate in hematopiesis and development of the brain during childhood. Whereas deficiency of AdCbl disturbs the carbohydrate, fat and amino-acid metabolism, and hence interferes with the formation of myelin. Thereby, it is important to treat vitamin B12 deficiency with a combination of MeCbl and AdCbl or Hydroxocobalamin or Cbl. Regarding the route, it has been proved that the oral route is comparable to the intramuscular route for rectifying vitamin B12 deficiency.

Hydroxocobalamin in cyanide poisoning

Clin Toxicol (Phila) 2012 Dec;50(10):875-85.PMID:23163594DOI:10.3109/15563650.2012.742197.

Introduction: On theoretical grounds, Hydroxocobalamin is an attractive antidote for cyanide poisoning as cobalt compounds have the ability to bind and detoxify cyanide. This paper reviews the pharmacokinetic and pharmacodynamic aspects of Hydroxocobalamin, its efficacy in human cyanide poisoning and its adverse effects. Methods: PubMed was searched for the period 1952 to April 2012. A total of 71 papers were identified in this way; and none was excluded. PHARMACOKINETICS AND PHARMACODYNAMICS: Pharmacokinetic studies in dogs and humans suggest a two-compartment model, with first order elimination kinetics. Pharmacodynamic studies in animals suggest that Hydroxocobalamin would be a satisfactory antidote for human cyanide poisoning. EFFICACY IN HUMAN POISONING: There is limited evidence that Hydroxocobalamin alone is effective in severe poisoning by cyanide salts. The evidence for the efficacy of Hydroxocobalamin in smoke inhalation is complicated by lack of evidence for the importance of cyanide exposure in fires and the effects of other chemicals as well as confounding effects of other therapeutic measures, including hyperbaric oxygen. Evidence that Hydroxocobalamin is effective in poisoning due to hydrogen cyanide alone is lacking; extrapolation of efficacy from poisoning by ingested cyanide salts may not be valid. The rate of absorption may be greater with inhaled hydrogen cyanide and the recommended slow intravenous administration of Hydroxocobalamin may severely limit its clinical effectiveness in these circumstances. Adverse effects: Both animal and human data suggest that Hydroxocobalamin is lacking in clinically significant adverse effects. However, in one human volunteer study, delayed but prolonged rashes were observed in one-sixth of subjects, appearing 7 to 25 days after administration of 5 g or more of Hydroxocobalamin. Rare adverse effects have included dyspnoea, facial oedema, and urticaria. Conclusions: Limited data on human poisonings with cyanide salts suggest that Hydroxocobalamin is an effective antidote; data from smoke inhalation are less clear-cut. Although clinically important reactions to Hydroxocobalamin have not been seen, some, non-life threatening, adverse reactions can occur.

High-Dose IV Hydroxocobalamin (Vitamin B12) in Septic Shock: A Double-Blind, Allocation-Concealed, Placebo-Controlled Single-Center Pilot Randomized Controlled Trial (The Intravenous Hydroxocobalamin in Septic Shock Trial)

Chest 2023 Feb;163(2):303-312.PMID:36174744DOI:10.1016/j.chest.2022.09.021.

Background: Elevated hydrogen sulfide (H2S) contributes to vasodilatation and hypotension in septic shock, and traditional therapies do not target this pathophysiologic mechanism. High-dose IV Hydroxocobalamin scavenges and prevents H2S formation, which may restore vascular tone and may accentuate recovery. No experimental human studies have tested high-dose IV Hydroxocobalamin in adults with septic shock. Research question: In adults with septic shock, is comparing high-dose IV Hydroxocobalamin with placebo feasible? Study design and methods: We conducted a phase 2 single-center, double-blind, allocation-concealed, placebo-controlled, parallel-group pilot randomized controlled trial comparing high-dose IV Hydroxocobalamin with placebo in critically ill adults with septic shock. Patients meeting Sepsis 3 criteria were randomized 1:1 to receive a single 5-g dose of high-dose IV Hydroxocobalamin or equivalent volume 0.9% saline solution as placebo. The primary outcome was study feasibility (enrollment rate, clinical and laboratory compliance rate, and contamination rate). Secondary outcomes included between-group differences in plasma H2S concentrations and vasopressor dose before and after infusion. Results: Twenty patients were enrolled over 19 months, establishing an enrollment rate of 1.05 patients per month. Protocol adherence rates were 100% with zero contamination. In the high-dose IV Hydroxocobalamin group, compared to placebo, there was a greater reduction in vasopressor dose between randomization and postinfusion (-36% vs 4%, P < .001) and randomization and 3-h postinfusion (-28% vs 10%, P = .019). In the high-dose IV Hydroxocobalamin group, the plasma H2S level was reduced over 45 mins by -0.80 ± 1.73 μM, as compared with -0.21 ± 0.64 μM in the placebo group (P = .3). Interpretation: This pilot trial established favorable feasibility metrics. Consistent with the proposed mechanism of benefit, high-dose IV Hydroxocobalamin compared with placebo was associated with reduced vasopressor dose and H2S levels at all time points and without serious adverse events. These data provide the first proof of concept for feasibility of delivering high-dose IV Hydroxocobalamin in septic shock. Trial registry: ClinicalTrials.gov; No.: NCT03783091; URL: www. Clinicaltrials: gov.

Hydroxocobalamin infusion in a patient monitored for plasma free hemoglobin levels

Clin Biochem 2022 Nov-Dec;109-110:94-97.PMID:36126746DOI:10.1016/j.clinbiochem.2022.09.008.

Hemolysis is one of the most common preanalytical concerns in the clinical laboratory. Hydroxocobalamin administration causes red pigmentation of plasma that may mimic hemolysis and may interfere with chemistry assays. A male patient in his sixties was placed on extracorporeal membrane oxygenation (ECMO) as a bridge to transplantation. Daily plasma free hemoglobin measurements were ordered to monitor for adverse ECMO events. An intensely red plasma specimen was inconsistent with modestly elevated hemoglobin levels and became pink on dilution. Follow-up with providers indicated that the red plasma could be attributed to Hydroxocobalamin administration. Performance of scanning spectrophotometry and assessment of a sample spiked with Hydroxocobalamin indicated that the red colored Hydroxocobalamin did not interfere with our 3,3',5,5'-tetramethylbenzidine based methodology for free plasma hemoglobin measurement. It is important for the laboratory professionals to be aware of the possibility of interference in hemoglobin assays due to Hydroxocobalamin.

Iatrogenic pediatric Hydroxocobalamin overdose

Am J Emerg Med 2019 Jul;37(7):1394.e1-1394.e2.PMID:31000316DOI:10.1016/j.ajem.2019.04.012.

Introduction: Hydroxocobalamin, a precursor molecule to vitamin B12, has emerged as the preferred empiric treatment for patients rescued from enclosed-space fires with concern for inhalational injury and potential concomitant cyanide toxicity. Limited data exist on the effects of Hydroxocobalamin toxicity, particularly in pediatric patients. Case report: We report a case of a healthy three-year old girl who was rescued from an apartment fire and electively intubated by prehospital providers. Due to concern for potential cyanide toxicity, she received 5 g (373 mg/kg) of intravenous Hydroxocobalamin, an amount equivalent to one standard adult dose but over five times the appropriate weight-adjusted dose for this 13.4-kilogram child. On hospital arrival, patient was noted to have chromaturia and diffuse erythroderma without cutaneous burns. She was extubated 4 h after prehospital intubation and discharged home the following morning in good condition with persistent erythroderma. Skin color returned to normal within two days. Discussion: We believe this to be the first reported case of iatrogenic pediatric Hydroxocobalamin overdose for the treatment of suspected cyanide toxicity. Erythroderma and chromaturia are expected side effects of Hydroxocobalamin, even at therapeutic levels. Along with minor airway burns, the only other finding was a transient and hemodynamically neutral bradycardia, which began shortly after prehospital intubation. As this bradycardia occurred prior to Hydroxocobalamin administration, more likely culprits include vagal nerve stimulation from direct laryngoscopy, and sinoatrial muscarinic receptor stimulation caused by repeated doses of succinylcholine. In all, we were unable to appreciate any complications due to excess Hydroxocobalamin administration.