Monocarboxylate Transporter
Monocarboxylates such as pyruvate, lactate, and the ketone bodies (acetoacetate and b-hydroxybutyrate) play essential roles in carbohydrate, fat, and amino acid metabolism and must be rapidly transported across the plasma membrane of cells. Transport is mediated by proton-linked monocarboxylate transporters (MCTs), four of which (MCTs1–4) have been characterized in detail. They are part of a family of transporter proteins, known as the MCT or SLC16 solute carrier family, that share characteristic sequence motifs. All family members are predicted to have 12-transmembrane helices (TMs) with intracellular C- and N-termini and a large cytosolic loop between TMs 6 and 7. As in other major facilitator superfamily members, the TM regions are more conserved than the loops and C-terminus. The MCT family has a total of 14 members whose predicted phylogeny, only MCTs1–4 have been confirmed to function as proton-linked MCTs. MCT10 was identified as an aromatic amino acid transporter originally called T-type amino acid transporter 1 (TAT1) and MCT8 shown to be an important thyroid hormone transporter. Transport mediated by MCT8 and MCT10 is not proton linked. The function of the other eight MCTs is unknown. In addition to their normal metabolic roles, MCTs may also be important for the transport of some drugs across the plasma membrane. There are also two distinct sodium-linked monocarboxylate transporters that are members of the SLC5 solute carrier family. These play a key role in endothelial monocarboxylate transport in the gut and kidney.
References
1.Halestrap AP. IUBMB Life. 2012;64(1):1–9.
References
1.Halestrap AP. IUBMB Life. 2012;64(1):1–9.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
Monocarboxylate Transporter
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Coumarin343
产品货号 : M36948
cas no: 55804-65-4
Coumarin 343 (C343) 是一种用于微水池的亲水性荧光探针。λem 约为 425 nm,λem 约为 425~550 nm (RF-1500)。 -
MCT1-IN-3
产品货号 : M35939
cas no: 2878360-80-4
MCT1-IN-3 是一种单羧酸转运蛋白 1 (MCT1) 抑制剂,IC50 值为 81.0 nM。MCT1-IN-3 还对多药转运蛋白 ABCB1 具有显著的抑制作用。MCT1-IN-3 可用于癌症的研究。 -
AZD0095
产品货号 : M35816
cas no: 2750001-23-9
AZD0095 是一种具有选择性和口服活性的 MCT4 抑制剂 (IC50: 1.3 nM)。 AZD0095 与 Cediranib (HY-10205) 联合使用可有效抑制 NCI-H358 移植瘤的肿瘤生长。 -
VB124
产品货号 : M35358
cas no: 2230186-18-0
VB124 是一种具有口服活性的、有效的、选择性的 MCT4 抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸涌入和流出,IC50 分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。 -
MSC-4381
产品货号 : M34984
cas no: 2445185-57-7
MSC-4381 (MCT4-IN-1) 是一种口服有效的,选择性的单羧酸转运蛋白 4 (MCT4/SLC16A3) 抑制剂,IC50 值为 77 nM,Ki 值为 11 nM。MSC-4381 靶向与 MCT4 的胞质域。MSC-4381 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MSC-4381 具有用于 MCT4 转运蛋白研究的潜力。