6385-02-0 Usage
Description
Meclofenamate is a time-dependent, non-specific competitive inhibitor of COX-1 and -2. The IC50 values for inhibition of human recombinant COX-1 and -2 are 1.5 and 9.7 μM, respectively for instantaneous inhibition. However, the IC50 is much lower if pre-incubated with the enzyme.
Uses
Different sources of media describe the Uses of 6385-02-0 differently. You can refer to the following data:
1. Meclofenamate Sodium is an NSAID used in the treatment of chronic pain.
2. antiinflammatory, antipyretic
Definition
ChEBI: An organic sodium salt derived from meclofenamic acid. Its monohydrate is used for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.
Indications
Meclofenamate sodium (Meclomen) is
prescribed for rheumatoid arthritis and osteoarthritis.
The fenamates show no clear superiority in antiinflammatory
activity and may produce more adverse
effects than other NSAIDs.
Therapeutic Function
Antiinflammatory
General Description
Meclofenamate sodium (Meclomen) is available for use inthe treatment of acute and chronic RA, OA, and primarydysmenorrhea. It is metabolized in a similar manner tomefenamic acid discussed above, thus a similar restriction isalso applied to meclofenamate. The most significant side effectsare GI, including diarrhea.
Pharmacokinetics
Meclofenamate sodium is rapidly and almost completely absorbed following oral administration, reaching peak plasma
levels within 2 hours. It is highly bound to plasma proteins (99%) and has a plasma half-life of 2 to 4 hours.
Metabolism involves oxidation of the methyl group, aromatic hydroxylation, monodehalogenation, and conjugation.
Urinary excretion accounts for approximately 75% of the administered dose. The major metabolite is the product of
3′-methyl oxidation and has been shown to possess anti-inflammatory activity.
Clinical Use
Meclofenamate sodium is indicated for the relief of mild to moderate pain, the acute and chronic treatment of
rheumatoid arthritis and osteoarthritis, the treatment of primary dysmenorrhea, and the treatment of idiopathic, heavy
menstrual blood loss.
Check Digit Verification of cas no
The CAS Registry Mumber 6385-02-0 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 6,3,8 and 5 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 6385-02:
(6*6)+(5*3)+(4*8)+(3*5)+(2*0)+(1*2)=100
100 % 10 = 0
So 6385-02-0 is a valid CAS Registry Number.
InChI:InChI=1/C14H11Cl2NO2.Na/c1-8-6-7-10(15)13(12(8)16)17-11-5-3-2-4-9(11)14(18)19;/h2-7,17H,1H3,(H,18,19);
6385-02-0Relevant articles and documents
Development and validation of a potent and specific inhibitor for the CLC-2 chloride channel
Koster, Anna K.,Reesec, Austin L.,Kuryshev, Yuri,Wen, Xianlan,McKiernana, Keri A.,Graya, Erin E.,Wu, Caiyun,Huguenard, John R.,Maduke, Merritt,Du Bois
, p. 32711 - 32721 (2020/12/30)
CLC-2 is a voltage-gated chloride channel that is widely expressed in mammalian tissues. In the central nervous system, CLC-2 appears in neurons and glia. Studies to define how this channel contributes to normal and pathophysiological function in the central nervous system raise questions that remain unresolved, in part due to the absence of precise pharmacological tools for modulating CLC-2 activity. Herein, we describe the development and optimization of AK-42, a specific small-molecule inhibitor of CLC-2 with nanomolar potency (IC50= 17 ± 1 nM). AK-42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and exhibits no off-target engagement against a panel of 61 common channels, receptors, and transporters expressed in brain tissue. Computational docking, validated by mutagenesis and kinetic studies, indicates that AK-42 binds to an extracellular vestibule above the channel pore. In electrophysiological recordings of mouse CA1 hippocampal pyramidal neurons, AK-42 acutely and reversibly inhibits CLC-2 currents; no effect on current is observed on brain slices taken from CLC-2 knockout mice. These results establish AK-42 as a powerful tool for investigating CLC-2 neurophysiology.
