free acid

Cholecystokinin (26-33) free acid, a part of cholecystokinin (CCK), is a highly selective ligand for CCKB-type receptors found in the vertebrate CNS and induces a mild taste aversion conditioned reflex in rats.

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.

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

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

Dimesna (BNP-778), when used in conjunction with active cancer chemotherapy agents, can reduce the toxicity associated with uremia.

Monophosphoryl lipid A (free acid) acts as an agonist for toll-like receptor 4. It is employed in immunological and vaccine research.

3D-Monophosphoryl Lipid A-5 (free acid) is a TLR agonist used as an adjuvant in vaccines to enhance their immunogenicity.

Monophosphoryl Lipid A-12 (free acid) functions as a toll-like receptor 4 agonist, primarily utilized in immunology and vaccine research.

BNC105P is a benzo[b]furan-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and anti-tumor effects. Upon administration, BNC105P, in its disodium phosphate form, rapidly converts to BNC105. In activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may block spindle formation, cause cell cycle arrest, and dismantle the tumor vasculature. This creates a hypoxic environment, depriving tumor cells of nutrients, leading to apoptosis. Apart from its VDA activity, BNC105P also exerts direct cytotoxic effects on tumor cells by inhibiting tubulin polymerization. Notably, BNC105 is not a substrate for the multidrug-resistant P-glycoprotein (Pgp) transporter.

3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) free acid is a TLR agonist that serves as a vaccine adjuvant to boost the immunogenicity of vaccines.

Prostaglandin I2 is an unstable prostaglandin compound that inhibits platelet aggregation and induces vasodilation in the pulmonary vasculature via the "I prostanoid" (IP) receptor. AFP 07, a 7,7-difluoroprostacyclin derivative, serves as a selective and potent agonist for the IP receptor (Ki=0.561 nM). It exhibits weaker affinity for EP receptors, with a Ki value of > 100 nM for EP1-3 and > 10 nM for EP4. The compound 16(R)-AFP 07 free acid is an enantiomer of AFP 07. Its biological properties, particularly those involving IP and EP receptors, are yet to be fully assessed.

EG01449 Free acid is a quinoline-based antagonist of neuropilin-1 (NRP1), exhibiting a Kd of 0.6 µM. It competitively inhibits the binding of VEGFA to NRP1, with an IC50 of 362 nM. By inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons, EG01449 Free acid prevents VEGFA-induced pain. Additionally, it is capable of crossing the blood-brain barrier, allowing for targeted effects within the central nervous system. EG01449 Free acid is applicable for pain research.

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

Fonsartan is an angiotensin receptor antagonist. Fonsartan inhibits the angiotensin II-induced trophic effects, fibronectin release and fibronectin-EIIIA+ expression in rat aortic vascular smooth muscle cells in vitro.

KRH-594 is a potent, specific and insurmountable AT1 receptor antagonist. KRH-594 ameliorates hyperlipidaemia and nephropathy in diabetic spontaneously hypertensive rats. KRH-594 prevents end-organ damage in stroke-prone spontaneously hypertensive/Izm ra

RDEA-806, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

SM19712 free acid is an inhibitor of nonpeptide endothelin converting enzyme.