PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors.IC50 value: 16 nMTarget: EP2in vitro: PF-04418948 inhibits prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent KB of 5.4 nM. [1]in vivo: In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Reversal of the PGE2-induced relaxation in the mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM. Given orally, PF-04418948 attenuated the butaprost-induced cutaneous blood flow response in rats. [1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively.[2]
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1].
Endotoxin inhibitor a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor inhibits the febrile response to LPS with very low toxicity and lethality[1].
Butofilolol is a potent β-blocking agent used in the research of hypertension[1].
L-Talose-13C-1 is the 13C labeled L-Talose[1].
pTH-Related Protein (1-37) (human, mouse, rat), the peptide analogue of pTH-Related Protein (pTHrP). pTHrP refers to parathyroid-hormone-related protein, involved in physiological regulation of bone formation[1].
Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
VU0152099 is a potent, selective, CNS-penetrant positive allosteric modulator of M4 mAChR with EC50 of 403 nM; shows no agonist activity but potentiates responses of M(4) to acetylcholine, and is devoid of activity at other mAChR subtypes or at a panel of other GPCRs; reverses amphetamine-induced hyperlocomotion in rats.
D-Nonamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Nonamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells[1].
Cassyfiline (Cassythine) is an aporphine alkaloid. Cassyfiline has potent vasorelaxing effects on precontracted rat aortic preparations with an IC50 of 0.09 μM[1].
Bederocin (REP8839) is a Methionyl-tRNA synthetase inhibitor. Bederocin can be used in research of bacterial infection, including S. aureus and MRSA[1].
Fmoc-HoCys(ACM)-OH, a homolog of cysteine, is synthesized from L-methionine. Fmoc-HoCys(ACM)-OH also can be used for the synthesis of solid phase peptide[1].
DDRI-18 is a DNA damage response inhibitor that inhibits the non-homologous end-joining (NHEJ) DNA repair process. DDRI-18 is an effective chemosensitizing agent[1].
Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB)[1].
Norcaesalpinin E is a natural cassane-type diterpene found in the seed kernels of Caesalpinia crista[1].
4-Allyltoluene, an aromatic compound, can elicite antennal olfactory response of Mediterranean fruit fly measured by electroantennography (EAG)[1].
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local anesthetic that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease[1].
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
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Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease[1].
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth[1].
Nonylbenzene-PEG5-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Benzyl-PEG1-Ms is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B[1].
8-Bromo-AMP (8-Bromoadenosine 5'-monophosphate) is a membrane permeable cAMP analogue. 8-Bromo-AMP can improve the ability of the heart to recover from ischemia and reperfusion by increasing the levels of ATP, ADP, and total adenine nucleotides[1][2].
(4α,11β,15β)-11,15-Dihydroxykaur-16-en-19-oic acid is a compound isolated from the Tunisian Pulicaria laciniata (Coss.et Kral.) Thell. flowers[1].
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID)[1].
Lactoferricin H, Lactotransferrin (37-61), human is a biological active peptide. (This is an antimicrobial peptide derived from human lactotransferrin amino acid residues 37-61.)
N-Acetyl-S-allyl-L-cysteine-d3 is the deuterium labeled Fluometuron[1].