free acid

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm Hg reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type prostaglandins; for example, prostaglandin F2α will produce this degree of miosis at a dose of less than 1 μg/eye.

IQ-1S free acid (IQ-1S) 是 NF-κB/激活蛋白1 (AP-1) 抑制剂(IC50:2.3±0.41 μM)。它对 JNK1(Kd:240 nM)、JNK2(Kd:360 nM) 和 JNK3(Kd:100 nM)的都具有高的结合亲和力 。

Cefpodoxime (free acid) 是一种口服的第三代头孢菌素抗生素。除铜绿假单胞菌、肠球菌和脆弱拟杆菌外，它对大多数革兰氏阳性和革兰氏阴性微生物均有效。

Cholecystokinin (26-33) free acid 是胆囊收缩素 (CCK) 的一部分， 是脊椎动物中枢神经系统中存在的 CCKB 型受体的高选择性配体，可诱导大鼠轻度味觉厌恶条件反射。

4-Methylumbelliferyl-α-L-Iduronide 是 α-L-艾杜糖醛酸酶催化活性常用底物。

Dianemycin (Nanchangmycin (free acid)) 由Streptomyces nanchangensis 产生的一种聚醚抗生素，抑制革兰氏阳性菌。它也是一种针对 Zika 病毒的广谱抗病毒药物。

GSK2983559 free acid 是一种有效的特异性受体相互作用蛋白 2 (RIP2) 抑制剂。 GSK2983559 free acid 在阻断人类炎症性肠病外植体样品和体内的许多促炎细胞因子反应方面表现出优异的活性。

AMI-1 free acid 是一种具有细胞渗透性和可逆的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂，具有潜在的抗癌活性，抑制 PRMT1 和酵母 Hmt1p，抑制精氨酸甲基化，调节来自雌激素和雄激素反应元件的核受体调节的转录。

AM095 free acid 是LPA1受体拮抗剂，对重组人和小鼠 LPA1 的IC50值分别为 0.98 和 0.73 μM。

SSR128129E free acid is an orally available and allosteric inhibitor of FGFR(IC50 of 1.9 μM for FGFR1).

Dimesna (BNP-778) 在与癌症化疗活性分子合用时，能有效减轻尿毒症的毒性。

Monophosphoryl lipid A (free acid) 是一种激活toll-like receptor 4的化合物，常用于免疫学和疫苗研究领域。

3D-Monophosphoryl Lipid A-5 (free acid) 作为一种有效的TLR激动剂，常用于疫苗中作为佐剂，用以提升疫苗的免疫原性。

Monophosphoryl Lipid A-12 free acid，作为一个toll-like receptor4激动剂，主要应用于免疫和疫苗研究领域。该化合物以Monophosphoryl Lipid A-12 (free acid)的形式活跃于相关生物医学研究中。

BNC105P是一种基于苯并呋喃的血管破坏剂(VDA)前体化合物，具有潜在的抗血管和抗肿瘤活性。当BNC105P被给药时，这种二钠磷酸酯形式的BNC105迅速转化为BNC105；在活化的内皮细胞中，BNC105与微管蛋白结合并抑制其聚合，这可能导致阻止纺锤体的形成、细胞周期阻滞以及破坏肿瘤的血管结构。随后形成缺氧状态，剥夺肿瘤细胞的营养供应，导致肿瘤细胞凋亡。除了其VDA活性外，BNC105P还通过抑制微管蛋白的聚合直接对肿瘤细胞产生细胞毒作用。值得注意的是，BNC105不是多药耐药P-糖蛋白(Pgp)转运体的底物。

3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) free acid 是一种作为疫苗佐剂的TLR激动剂，能够增强疫苗的免疫原性。

Prostaglandin I2 是一种不稳定的前列腺素，借助“I 前列腺素类物质”(IP) 受体来抑制血小板聚集并促进肺血管床的血管扩张。AFP 07 是一种 7,7-二氟前列环素衍生物，充当 IP 受体的选择性高效激动剂 (Ki=0.561 nM)。在EP受体上，AFP 07 的亲和力相对较弱，对 EP1-3 的 Ki 值大于 100 nM，对 EP4 的 Ki 值大于 10 nM。16(R)-AFP 07 free acid 是其差向异构体，其在生物学特性上（尤其是通过 IP 和 EP 受体）仍需进一步研究。

AFP 07 free acid is a 7,7-difluoroprostacyclin derivative. It also acts as a selective and highly potent agonist for the IP receptor.

Gastrazole is a CCK2 receptor antagonist potentially. It also used for the treatment of pancreatic cancer.

OSI-7904L is a folate-based thymidylate synthase inhibitor. It also has antimalarial and antitumor properties.

EC17 is a FITC conjugated folic acid, also known as Folate-FITC. It also acts as an FRα-targeting agent that fluoresces at 500nm. EC17 is a conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic acti

E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr

FK-739 is an angiotensin type 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensin II to bovine cerebel