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拉科酰胺

规格或纯度: 98%
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货号 (SKU) 包装规格 是否现货 价格 数量
L125374-10mg 10mg 现货 Stock Image
L125374-25mg 25mg 现货 Stock Image
L125374-50mg 50mg 现货 Stock Image
L125374-250mg 250mg 期货 Stock Image
L125374-1g 1g 现货 Stock Image
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Nav1.2 Channel blocker Nav1.3 Channel blocker Nav1.7 Channel blocker Nav1.8 Channel blocker
main product photo

基本描述

规格或纯度 98%
英文名称 Lacosamide
别名 拉科酰胺；(R)-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺；N2-乙酰基-N-苄基-O-甲基-D-丝氨酰胺
英文别名 Vimpat; Erlosamide;(R)-2-Acetamido-N-benzyl-3-methoxypropanamide；N2-Acetyl-N-benzyl-O-methyl-D-serinamide
生化机理 Lacosamide is a functionalized amino acid that produces activity in the maximal electroshock seizure (MES) test, that, like some other antiepileptic drμgs (AEDs), are believed to act throμgh voltage-gated sodium channels. Lacosamide enhances the slow inactivation of voltage-gated sodium channels without affecting the fast inactivation of voltage-gated sodium channels. This inactivation prevents the channel from opening, helping end the action potential. Many antiepileptic drμgs, like carbamazepine or lamotrigine, slow the recovery from inactivation and hence reduce the ability of neurons to fire action potentials.
储存温度 -20°C储存,充氩
运输条件 超低温冰袋运输
备注 50mg、25mg卖完停产，不再备货
产品介绍

Lacosamide (Vimpat; Erlosamide)可作用于部分发作的癫痫和糖尿病引发的神经性疼痛。

Lacosamide (Vimpat; Erlosamide) is a medication developed for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain.

名称和标识符

IUPAC Name (2R)-2-acetamido-N-benzyl-3-methoxypropanamide
INCHI InChI=1S/C13H18N2O3/c1-10(16)15-12(9-18-2)13(17)14-8-11-6-4-3-5-7-11/h3-7,12H,8-9H2,1-2H3,(H,14,17)(H,15,16)/t12-/m1/s1
InChi Key VPPJLAIAVCUEMN-GFCCVEGCSA-N
Canonical SMILES CC(=O)NC(COC)C(=O)NCC1=CC=CC=C1
分子式

C13H18N2O3
PubChem CID 219078
分子量 250.29

化学和物理性质

溶解性 DMSO ≥48mg/mL Water ≥24mg/mL Ethanol ≥48mg/mL
敏感性 热敏感；对空气敏感
闪点(℉) 35.6?°F
闪点(℃) 35.6°F

安全信息

象形图
ghs06

Toxic

ghs07

Harmful
信号词 Danger
危险声明 H319: Causes serious eye irritation
H301: Toxic if swallowed
预防措施声明 P305+P351+P338,P280,P321,P405,P501,P264,P270,P330,P264+P265,P301+P316,P337+P317
WGK Germany 2

靶标

Target ID 579
名称 Nav1.2
缩写名 SHP2
家族 Voltage-gated sodium channels (NaV)
别名 CC CKR5
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 24 2005 2q24.3 SCN2A sodium voltage-gated channel alpha subunit 2
Rat 24 2005 3q21 Scn2a sodium voltage-gated channel alpha subunit 2
Mouse 24 2006 2 C1.3 Scn2a sodium channel, voltage-gated, type II, alpha
OMIM 182390 (Hs)
Entrez Gene 24766 (Rn) , 110876 (Mm) , 6326 (Hs)
UniProtKB P04775 (Rn) , Q99250 (Hs)
RefSeq Protein NP_036779 (Rn) , NP_001092768 (Mm) , NP_001035233 (Hs) , NP_001035232 (Hs)
RefSeq Nucleotide NM_012647 (Rn) , NM_001099298 (Mm) , NM_001040143 (Hs) , NM_001040142 (Hs)
Ensembl Gene ENSG00000136531 (Hs) , ENSMUSG00000075318 (Mm) , ENSRNOG00000005018 (Rn)
Orphanet 118500 (Hs)
Protein GI 6981506 (Rn) , 93141214 (Hs) , 150010574 (Mm)
DrugBank Target Q99250 (Hs)
ChEMBL Target CHEMBL3399 (Rn) , CHEMBL4187 (Hs)
Target ID 580
名称 Nav1.3
缩写名 SHP2
家族 Voltage-gated sodium channels (NaV)
别名 CC CKR5
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 24 2000 2q24.3 SCN3A sodium voltage-gated channel alpha subunit 3
Rat 24 1951 3q21 Scn3a sodium voltage-gated channel alpha subunit 3
Mouse 24 1947 2 C1.3 Scn3a sodium channel, voltage-gated, type III, alpha
OMIM 182391 (Hs)
Entrez Gene 20269 (Mm) , 497770 (Rn) , 6328 (Hs)
UniProtKB Q9NY46 (Hs) , P08104 (Rn)
RefSeq Protein NP_008853 (Hs) , NP_037251 (Rn) , NP_061202 (Mm)
RefSeq Nucleotide NM_006922 (Hs) , NM_013119 (Rn) , NM_018732 (Mm)
Ensembl Gene ENSG00000153253 (Hs) , ENSMUSG00000057182 (Mm) , ENSRNOG00000005007 (Rn)
Protein GI 6981510 (Rn) , 126362955 (Hs) , 160707887 (Mm)
DrugBank Target Q9NY46 (Hs)
ChEMBL Target CHEMBL5163 (Hs) , CHEMBL4966 (Rn)
Target ID 584
名称 Nav1.7
缩写名 SHP2
家族 Voltage-gated sodium channels (NaV)
别名 CC CKR5
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 24 1988 2q24.3 SCN9A sodium voltage-gated channel alpha subunit 9
Rat 24 1984 3q21 Scn9a sodium voltage-gated channel alpha subunit 9
Mouse 24 1984 2 39.13 cM Scn9a sodium channel, voltage-gated, type IX, alpha
OMIM 603415 (Hs)
Entrez Gene 78956 (Rn) , 20274 (Mm) , 6335 (Hs)
UniProtKB Q62205 (Mm) , Q15858 (Hs) , O08562 (Rn)
RefSeq Protein NP_002968 (Hs) , NP_579823 (Rn) , NP_001277603 (Mm)
RefSeq Nucleotide NM_002977 (Hs) , NM_133289 (Rn) , NM_001290674 (Mm)
Ensembl Gene ENSG00000169432 (Hs) , ENSMUSG00000075316 (Mm) , ENSRNOG00000006639 (Rn)
Orphanet 118525 (Hs)
Protein GI 18959222 (Rn) , 594591612 (Mm) , 4506813 (Hs)
DrugBank Target Q15858 (Hs)
ChEMBL Target CHEMBL3312 (Rn) , CHEMBL3414411 (Mm) , CHEMBL4296 (Hs)
Target ID 585
名称 Nav1.8
缩写名 SHP2
家族 Voltage-gated sodium channels (NaV)
别名 CC CKR5
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 24 1956 3p22.2 SCN10A sodium voltage-gated channel alpha subunit 10
Rat 24 1956 8q32 Scn10a sodium voltage-gated channel alpha subunit 10
Mouse 24 1958 9 71.33 cM Scn10a sodium channel, voltage-gated, type X, alpha
OMIM 604427 (Hs)
Entrez Gene 20264 (Mm) , 29571 (Rn) , 6336 (Hs)
UniProtKB Q62968 (Rn) , Q6QIY3 (Mm) , Q9Y5Y9 (Hs)
RefSeq Protein NP_006505 (Hs) , NP_058943 (Rn) , NP_033160 (Mm)
RefSeq Nucleotide NM_006514 (Hs) , NM_017247 (Rn) , NM_009134 (Mm)
Ensembl Gene ENSG00000185313 (Hs) , ENSMUSG00000034533 (Mm) , ENSRNOG00000032473 (Rn)
Protein GI 8394242 (Rn) , 328927029 (Mm) , 110835710 (Hs)
Orphanet 325976 (Hs)
DrugBank Target Q9Y5Y9 (Hs)
ChEMBL Target CHEMBL5451 (Hs) , CHEMBL4017 (Rn) , CHEMBL5158 (Mm)

关联配体

Ligand ID 7472
名称 lacosamide
别名 erlosamide
类别 Synthetic organic
学名 (2R)-2-acetamido-3-methoxy-N-(phenylmethyl)propanamide
生物活性评价 We have tagged the Nav1.7 voltage-gated sodium channel as the primary target of this drug, simply as this is the only human voltage-gated sodium channel for which we have been able to find affinity data. This does not preclude interaction at other sodium channels.
评价 Lacosamide is a functionalized amino acid anticonvulsant drug .

参考文献

1. Sheets PL, Heers C, Stoehr T, Cummins TR.  (2008)  Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine..  J Pharmacol Exp Ther,  326  (1):  (89-99).  [PMID:18378801]
2. Beyreuther BK, Freitag J, Heers C, Krebsf?nger N, Scharfenecker U, St?hr T.  (2007)  Lacosamide: a review of preclinical properties..  CNS Drug Rev,  13  (1):  (21-42).  [PMID:17461888]

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