Pancreatic polypeptide is a peptide secreted by the endocrine PP cells of the pancreas that regulates pancreatic secretory activity and also affects hepatic glycogen stores and gastrointestinal secretion[1].
Gly-Leu-Met-NH2 is a C-terminal tripeptide of Substance P (Substance P (HY-P0201)). Substance P is a neuropeptide[1].
Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.IC50 value: 10 to 10,000 nM (Ki)Target: nAChR, mAChRCarbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR). Carbamoylcholine is an agonist of both nicotinic (nAChR) and muscarinic (mAChR) receptors, with reported Ki values ranging from 10 to 10,000 nM for different receptors and different preparations.
Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively[1].
Atosiban(RW22164; Tractocile) is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane.IC50 value:Target: As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua.[1][2] In human pre-term labour, atosiban, at the recommended dosage, antagonises uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].
N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research[1][2][3].
THX-B is a potent and non-peptidic p75NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders[1][2][3].
Piperoxan hydrochloride is an α2 adrenoceptor antagonist.
Ethyl linolenate is a fatty acid ethyl ester (FAEE). Ethyl linolenate plays an active role in inhibition of the cellular production on melanin with an IC50 of 70 μM. Anti-melanogenesis Effects[1].
AZD 1678 is a potent, selective orally bioavailable CCR4 receptor antagonist with pIC50 of 8.6 for hCCR4, pIC50 of 9.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.8. Asthma Phase 1 Clinical
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates[1][2][3][4].
BRL-15572 2Hcl is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. IC50 Value: 7.9(pKi)Target: 5-HT1D Receptorin vitro: BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 μM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors.in vivo: In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572.
Anisotropine methobromide is an orally active anticholinergic muscarinic antagonist. Anisotropine methobromide can inhibit gastric acid secretion and is used as an adjunct to peptic ulcers[1].
KRAS G12C inhibitor 24 is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 24 inhibits KRAS G12C/SOS1 interaction with an IC50 of＜50 nM (CN113563323A, compound 1)[1].
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19[1][2][3][4].
TIPP is a potent and selective δ-opioid antagonist with a Ki value of 1.22 nM[1].
Pizotifen malate is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
β2AR/M3-receptor agonist-1 (example 9) is a potent β2AR and M3 receptor agonist. β2AR/M3-receptor agonist-1 shows M3 receptor affinity with a pIC50 value of 9.3. β2AR/M3-receptor agonist-1 has the potential for the research of respiratory tract disorders[1].
Cortisone is a 21-carbon steroid hormone. Cortisone is one of the main hormones released by the adrenal gland in response to stress. Target： In chemical structure, it is a corticosteroid closely related to cortisol. It is used to treat a variety of ailments and can be administered intravenously, orally,intraarticularly (into a joint), or transcutaneously. Cortisone suppresses the immune system, thus reducing inflammation and attendant pain and swelling at the site of the injury. Risks exist, in particular in the long-term use of cortisone. Cortisone, a glucocorticoid, and adrenaline are the main hormones released by the body as a reaction to stress. They elevate blood pressure and prepare the body for a fight or flight response.
EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. EP4-IN-1 is extracted from patent WO2023025270 (example 1), and exhibits prospect in tumor immunity and anti-inflammatory analgesia research[1].
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research[1].
Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation[1][2].